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MK 2206 dihydrochloride

MK 2206 dihydrochloride

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商品描述
MK 2206 dihydrochloride:
Description

MK 2206 is an orally active allosteric Akt inhibitor with IC50s of 5, 12 and 65 nM for Akt1, Akt2 and Akt3, respectively.

IC50 & Target[1]

Akt1

5 nM (IC50)

Akt2

12 nM (IC50)

Akt3

65 nM (IC50)

Autophagy

 

In Vitro

The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 are treated with increasing doses of MK-2206 (0-10 μM) for 72 and 96 hours, results in dose- and time-dependent inhibition of cell viability. At 72 and 96 hours, the IC50 values of MK-2206 in CNE-1, CNE-2, and HONE-1 cell lines are 3-5 μM, and in SUNE-1, they are less than 1 μM. MK-2206 alone more potently inhibits the cell growth of Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292; IC50s of 5.5, 4.3, and 5.2 μM, respectively) as compared with Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6; IC50s of 13.5, 14.1, 27.0, and 28.6 μM, respectively), with the exception of NCI-H460, which has a PIK3CA E545K mutation (IC50, 3.4 μM).

In Vivo

MK-2206 doses (480 mg/kg once a week and 240 mg/kg three times a week) can inhibit the growth of human CNE-2 xenografts in nude mice. In the two MK-2206 groups, the tumor weights are much lighter than the control group (P<0.01). Temporal body weight reduction is observed after receiving the MK-2206 treatment.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01519427 National Cancer Institute (NCI) Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma January 2012 Phase 2
NCT01243762 Merck Sharp & Dohme Corp. Neoplasms Malignant November 22, 2010 Phase 1
NCT01239355 National Cancer Institute (NCI) Adult Hepatocellular Carcinoma|Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma December 2010 Phase 2
NCT01283035 National Cancer Institute (NCI) Ovarian Sarcoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma April 2011 Phase 2
NCT01239342 National Cancer Institute (NCI)|M.D. Anderson Cancer Center Metastatic Renal Cell Cancer|Recurrent Renal Cell Carcinoma|Stage IV Renal Cell Cancer January 27, 2011 Phase 2
NCT01186705 Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp. Colon Cancer|Rectal Cancer August 2010 Phase 2
NCT01349933 National Cancer Institute (NCI) Recurrent Squamous Cell Carcinoma of the Nasopharynx|Stage IV Squamous Cell Carcinoma of the Nasopharynx April 2011 Phase 2
NCT01295632 Merck Sharp & Dohme Corp. Advanced Cancer February 2011 Phase 1
NCT01231919 National Cancer Institute (NCI) Accelerated Phase Chronic Myelogenous Leukemia|Acute Leukemias of Ambiguous Lineage|Acute Myeloid Leukemia+Transient Myeloproliferative Disorder|Acute Undifferentiated Leukemia|Aggressive NK-cell Leukemia|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Blastic Phase Chronic Myelogenous Leukemia|Blastic Plasmacytoid Dendritic Cell Neoplasm|Childhood Burkitt Lymphoma|Childhood Chronic Myelogenous Leukemia|Childhood Diffuse Large Cell Lymphoma|Childhood Grade III Lymphomatoid Granulomatosis|Childhood Immunoblastic Large Cell Lymphoma|Childhood Nasal Type Extranodal NK+T-cell Lymphoma|Chronic Eosinophilic Leukemia|Chronic Myelomonocytic Leukemia|Chronic Neutrophilic Leukemia|Chronic Phase Chronic Myelogenous Leukemia|Intraocular Lymphoma|Juvenile Myelomonocytic Leukemia|Mast Cell Leukemia|Myeloid+NK-cell Acute Leukemia|Noncutaneous Extranodal Lymphoma|Post-transplant Lymphoproliferative Disorder|Primary Central Nervous System Hodgkin Lymphoma|Primary Central Nervous System Non-Hodgkin Lymphoma|Progressive Hairy Cell Leukemia, Initial Treatment|Prolymphocytic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Recurrent Childhood Anaplastic Large Cell Lymphoma|Recurrent Childhood Grade III Lymphomatoid Granulomatosis|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides+Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Recurrent+Refractory Childhood Hodgkin Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Hairy Cell Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Unspecified Childhood Solid Tumor, Protocol Specific|Waldenström Macroglobulinemia January 2011 Phase 1
NCT01333475 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Colorectal Neoplasms March 2011 Phase 2
NCT01239355 National Cancer Institute (NCI) Adult Hepatocellular Carcinoma|Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma December 2010 Phase 2
NCT01277757 National Cancer Institute (NCI) Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer March 2011 Phase 2
NCT01021748 Merck Sharp & Dohme Corp.|AstraZeneca Locally Advanced or Metastatic Solid Tumors November 23, 2009 Phase 1
NCT01370070 Chinese University of Hong Kong Recurrent Nasopharyngeal Carcinoma July 2011 Phase 2
NCT01240941 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer February 2011 Phase 2
NCT01248247 M.D. Anderson Cancer Center|Merck Sharp & Dohme Corp.|National Cancer Institute (NCI)|GlaxoSmithKline|Novartis Lung Cancer June 2011 Phase 2
NCT01658943 National Cancer Institute (NCI) Pancreatic Acinar Cell Carcinoma|Pancreatic Ductal Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage IV Pancreatic Cancer August 2012 Phase 2
NCT01306045 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic February 26, 2011 Phase 2
NCT01021748 Merck Sharp & Dohme Corp.|AstraZeneca Locally Advanced or Metastatic Solid Tumors November 23, 2009 Phase 1
NCT01294306 National Cancer Institute (NCI) Adenosquamous Lung Carcinoma|Bronchioloalveolar Carcinoma|Large Cell Lung Carcinoma|Lung Adenocarcinoma|Recurrent Non-Small Cell Lung Carcinoma|Squamous Cell Lung Carcinoma February 2011 Phase 2
NCT01248247 M.D. Anderson Cancer Center|Merck Sharp & Dohme Corp.|National Cancer Institute (NCI)|GlaxoSmithKline|Novartis Lung Cancer June 2011 Phase 2
NCT01277757 National Cancer Institute (NCI) Recurrent Breast Carcinoma|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer March 2011 Phase 2
NCT01231919 National Cancer Institute (NCI) Accelerated Phase Chronic Myelogenous Leukemia|Acute Leukemias of Ambiguous Lineage|Acute Myeloid Leukemia+Transient Myeloproliferative Disorder|Acute Undifferentiated Leukemia|Aggressive NK-cell Leukemia|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Blastic Phase Chronic Myelogenous Leukemia|Blastic Plasmacytoid Dendritic Cell Neoplasm|Childhood Burkitt Lymphoma|Childhood Chronic Myelogenous Leukemia|Childhood Diffuse Large Cell Lymphoma|Childhood Grade III Lymphomatoid Granulomatosis|Childhood Immunoblastic Large Cell Lymphoma|Childhood Nasal Type Extranodal NK+T-cell Lymphoma|Chronic Eosinophilic Leukemia|Chronic Myelomonocytic Leukemia|Chronic Neutrophilic Leukemia|Chronic Phase Chronic Myelogenous Leukemia|Intraocular Lymphoma|Juvenile Myelomonocytic Leukemia|Mast Cell Leukemia|Myeloid+NK-cell Acute Leukemia|Noncutaneous Extranodal Lymphoma|Post-transplant Lymphoproliferative Disorder|Primary Central Nervous System Hodgkin Lymphoma|Primary Central Nervous System Non-Hodgkin Lymphoma|Progressive Hairy Cell Leukemia, Initial Treatment|Prolymphocytic Leukemia|Recurrent Childhood Acute Lymphoblastic Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Recurrent Childhood Anaplastic Large Cell Lymphoma|Recurrent Childhood Grade III Lymphomatoid Granulomatosis|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides+Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Recurrent+Refractory Childhood Hodgkin Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Hairy Cell Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Unspecified Childhood Solid Tumor, Protocol Specific|Waldenström Macroglobulinemia January 2011 Phase 1
NCT01251861 National Cancer Institute (NCI) Recurrent Prostate Carcinoma|Stage I Prostate Cancer AJCC v7|Stage IIA Prostate Cancer AJCC v7|Stage IIB Prostate Cancer AJCC v7|Stage III Prostate Cancer AJCC v7 December 23, 2010 Phase 2
NCT01245205 National Cancer Institute (NCI) HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Unspecified Adult Solid Tumor, Protocol Specific November 2010 Phase 1
NCT01260701 National Cancer Institute (NCI) Adenocarcinoma of the Gastroesophageal Junction|Diffuse Gastric Adenocarcinoma|Gastric Intestinal Type Adenocarcinoma|Gastric Mixed Adenocarcinoma|Recurrent Gastric Carcinoma January 2011 Phase 2
NCT01235897 University of California, San Francisco|Merck Sharp & Dohme Corp. Advanced Solid Tumors|Tumors|Cancer March 2011 Phase 1
NCT01425879 National Cancer Institute (NCI) Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma|Recurrent Gallbladder Carcinoma|Stage IV Distal Bile Duct Cancer|Stage IV Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Carcinoma|Unresectable Gallbladder Carcinoma April 2011 Phase 2
NCT01859182 National Cancer Institute (NCI) Adenocarcinoma of the Gallbladder|Adenocarcinoma With Squamous Metaplasia of the Gallbladder|Adult Primary Cholangiocellular Carcinoma|Advanced Adult Primary Liver Cancer|Cholangiocarcinoma of the Extrahepatic Bile Duct|Localized Unresectable Adult Primary Liver Cancer|Metastatic Extrahepatic Bile Duct Cancer|Recurrent Adult Primary Liver Cancer|Recurrent Extrahepatic Bile Duct Cancer|Stage II Gallbladder Cancer|Stage IIIA Gallbladder Cancer|Stage IIIB Gallbladder Cancer|Stage IVA Gallbladder Cancer|Stage IVB Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Cancer January 2013 Phase 2
NCT01480154 National Cancer Institute (NCI) Adult Solid Neoplasm|Hormone-Resistant Prostate Carcinoma|Recurrent Melanoma|Recurrent Prostate Carcinoma|Recurrent Renal Cell Carcinoma|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Prostate Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 November 23, 2011 Phase 1
NCT01281163 National Cancer Institute (NCI) Estrogen Receptor Negative|Estrogen Receptor Positive|HER2+Neu Positive|Progesterone Receptor Negative|Progesterone Receptor Positive|Recurrent Breast Carcinoma|Stage IV Breast Cancer January 2011 Phase 1
NCT01307631 National Cancer Institute (NCI) Endometrial Adenocarcinoma|Endometrial Adenosquamous Carcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Serous Adenocarcinoma|Recurrent Uterine Corpus Carcinoma March 2011 Phase 2
NCT01349933 National Cancer Institute (NCI) Recurrent Squamous Cell Carcinoma of the Nasopharynx|Stage IV Squamous Cell Carcinoma of the Nasopharynx April 2011 Phase 2
NCT01258998 National Cancer Institute (NCI) Adult Nasal Type Extranodal NK+T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|B-cell Adult Acute Lymphoblastic Leukemia|B-cell Chronic Lymphocytic Leukemia|Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Hepatosplenic T-cell Lymphoma|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Noncutaneous Extranodal Lymphoma|Peripheral T-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia+Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides+Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Hairy Cell Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|T-cell Adult Acute Lymphoblastic Leukemia|T-cell Large Granular Lymphocyte Leukemia|Testicular Lymphoma|Waldenström Macroglobulinemia December 2010 Phase 2
NCT01370070 Chinese University of Hong Kong Recurrent Nasopharyngeal Carcinoma July 2011 Phase 2
NCT01240941 Vanderbilt-Ingram Cancer Center Metastatic Breast Cancer February 2011 Phase 2
NCT01519427 National Cancer Institute (NCI) Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma January 2012 Phase 2
NCT01071018 Merck Sharp & Dohme Corp. Solid Tumors February 2010 Phase 1
NCT01859182 National Cancer Institute (NCI) Adenocarcinoma of the Gallbladder|Adenocarcinoma With Squamous Metaplasia of the Gallbladder|Adult Primary Cholangiocellular Carcinoma|Advanced Adult Primary Liver Cancer|Cholangiocarcinoma of the Extrahepatic Bile Duct|Localized Unresectable Adult Primary Liver Cancer|Metastatic Extrahepatic Bile Duct Cancer|Recurrent Adult Primary Liver Cancer|Recurrent Extrahepatic Bile Duct Cancer|Stage II Gallbladder Cancer|Stage IIIA Gallbladder Cancer|Stage IIIB Gallbladder Cancer|Stage IVA Gallbladder Cancer|Stage IVB Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Cancer January 2013 Phase 2
NCT01369849 National Cancer Institute (NCI) Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia September 2011 Phase 1|Phase 2
NCT01480154 National Cancer Institute (NCI) Adult Solid Neoplasm|Hormone-Resistant Prostate Carcinoma|Recurrent Melanoma|Recurrent Prostate Carcinoma|Recurrent Renal Cell Carcinoma|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Prostate Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 November 23, 2011 Phase 1
NCT01042379 QuantumLeap Healthcare Collaborative Breast Neoplasms|Breast Cancer|Breast Tumors March 2010 Phase 2
NCT01705340 National Cancer Institute (NCI) Adenocarcinoma of the Gastroesophageal Junction|HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Recurrent Esophageal Cancer|Recurrent Gastric Cancer|Stage IIIC Breast Cancer|Stage IIIC Esophageal Cancer|Stage IIIC Gastric Cancer|Stage IV Breast Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer September 2012 Phase 1
NCT01369849 National Cancer Institute (NCI) Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia September 2011 Phase 1|Phase 2
NCT00670488 Merck Sharp & Dohme Corp. Locally Advanced Tumors|Metastatic Solid Tumors|Cancer|Neoplasms April 2008 Phase 1
NCT00848718 Merck Sharp & Dohme Corp. Locally Advanced, Metastatic Solid Tumors March 2009 Phase 1
NCT01147211 National Taiwan University Hospital Non Small Cell Lung Cancer September 2010 Phase 1
NCT01263145 National Cancer Institute (NCI) Adult Solid Neoplasm|Recurrent Breast Carcinoma|Stage IV Breast Cancer January 5, 2011 Phase 1
NCT01776008 National Cancer Institute (NCI) Estrogen Receptor Positive|HER2+Neu Negative|Recurrent Breast Carcinoma|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer January 2013 Phase 2
NCT01658943 National Cancer Institute (NCI) Pancreatic Acinar Cell Carcinoma|Pancreatic Ductal Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage IV Pancreatic Cancer August 2012 Phase 2
NCT01169649 Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp. PANCREAS|Neuroendocrine July 2010 Phase 2
NCT01253447 National Cancer Institute (NCI) Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia October 2010 Phase 2
NCT01425879 National Cancer Institute (NCI) Advanced Adult Hepatocellular Carcinoma|Localized Non-Resectable Adult Liver Carcinoma|Recurrent Adult Liver Carcinoma|Recurrent Gallbladder Carcinoma|Stage IV Distal Bile Duct Cancer|Stage IV Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Carcinoma|Unresectable Gallbladder Carcinoma April 2011 Phase 2
NCT01783171 National Cancer Institute (NCI) Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IV Pancreatic Cancer AJCC v6 and v7|Unresectable Pancreatic Carcinoma January 15, 2013 Phase 1
NCT01306045 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Carcinoma, Non-Small-Cell Lung|Carcinoma, Small Cell Lung|Carcinoma, Thymic February 26, 2011 Phase 2
NCT00670488 Merck Sharp & Dohme Corp. Locally Advanced Tumors|Metastatic Solid Tumors|Cancer|Neoplasms April 2008 Phase 1
NCT01249105 Dana-Farber Cancer Institute|Brigham and Women´s Hospital|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Memorial Sloan Kettering Cancer Center|University of California, Los Angeles|Merck Sharp & Dohme Corp. Malignant Glioma Phase 2
NCT01466868 Centre Leon Berard|National Cancer Institute, France Diffuse Large B Cell Lymphoma November 2011 Phase 2
NCT01783171 National Cancer Institute (NCI) Pancreatic Adenocarcinoma|Recurrent Pancreatic Carcinoma|Stage III Pancreatic Cancer AJCC v6 and v7|Stage IV Pancreatic Cancer AJCC v6 and v7|Unresectable Pancreatic Carcinoma January 15, 2013 Phase 1
NCT01239342 National Cancer Institute (NCI)|M.D. Anderson Cancer Center Metastatic Renal Cell Cancer|Recurrent Renal Cell Carcinoma|Stage IV Renal Cell Cancer January 27, 2011 Phase 2
NCT01186705 Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp. Colon Cancer|Rectal Cancer August 2010 Phase 2
NCT01604772 National Cancer Institute (NCI) Recurrent Oral Cavity Adenoid Cystic Carcinoma|Recurrent Salivary Gland Carcinoma|Salivary Gland Adenoid Cystic Carcinoma|Stage IVA Major Salivary Gland Cancer AJCC v7|Stage IVA Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7|Stage IVB Major Salivary Gland Cancer AJCC v7|Stage IVB Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7|Stage IVC Major Salivary Gland Cancer AJCC v7|Stage IVC Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7 July 23, 2012 Phase 2
NCT00963547 Merck Sharp & Dohme Corp. Advanced Solid Tumors|Breast Cancer September 15, 2009 Phase 1
NCT01333475 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Colorectal Neoplasms March 2011 Phase 2
NCT01258998 National Cancer Institute (NCI) Adult Nasal Type Extranodal NK+T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|B-cell Adult Acute Lymphoblastic Leukemia|B-cell Chronic Lymphocytic Leukemia|Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Hepatosplenic T-cell Lymphoma|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Noncutaneous Extranodal Lymphoma|Peripheral T-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia+Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides+Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Hairy Cell Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|T-cell Adult Acute Lymphoblastic Leukemia|T-cell Large Granular Lymphocyte Leukemia|Testicular Lymphoma|Waldenström Macroglobulinemia December 2010 Phase 2
NCT01251861 National Cancer Institute (NCI) Recurrent Prostate Carcinoma|Stage I Prostate Cancer AJCC v7|Stage IIA Prostate Cancer AJCC v7|Stage IIB Prostate Cancer AJCC v7|Stage III Prostate Cancer AJCC v7 December 23, 2010 Phase 2
NCT01776008 National Cancer Institute (NCI) Estrogen Receptor Positive|HER2+Neu Negative|Recurrent Breast Carcinoma|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer January 2013 Phase 2
NCT01042379 QuantumLeap Healthcare Collaborative Breast Neoplasms|Breast Cancer|Breast Tumors March 2010 Phase 2
NCT01319539 National Cancer Institute (NCI) Estrogen Receptor Negative|Estrogen Receptor Positive|HER2+Neu Negative|HER2+Neu Positive|Progesterone Receptor Negative|Progesterone Receptor Positive|Stage IA Breast Cancer|Stage IB Breast Cancer|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-Negative Breast Carcinoma April 2011 Phase 2
NCT00848718 Merck Sharp & Dohme Corp. Locally Advanced, Metastatic Solid Tumors March 2009 Phase 1
NCT01604772 National Cancer Institute (NCI) Recurrent Oral Cavity Adenoid Cystic Carcinoma|Recurrent Salivary Gland Carcinoma|Salivary Gland Adenoid Cystic Carcinoma|Stage IVA Major Salivary Gland Cancer AJCC v7|Stage IVA Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7|Stage IVB Major Salivary Gland Cancer AJCC v7|Stage IVB Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7|Stage IVC Major Salivary Gland Cancer AJCC v7|Stage IVC Oral Cavity Adenoid Cystic Carcinoma AJCC v6 and v7 July 23, 2012 Phase 2
NCT01243762 Merck Sharp & Dohme Corp. Neoplasms Malignant November 22, 2010 Phase 1
NCT01705340 National Cancer Institute (NCI) Adenocarcinoma of the Gastroesophageal Junction|HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Recurrent Esophageal Cancer|Recurrent Gastric Cancer|Stage IIIC Breast Cancer|Stage IIIC Esophageal Cancer|Stage IIIC Gastric Cancer|Stage IV Breast Cancer|Stage IV Esophageal Cancer|Stage IV Gastric Cancer September 2012 Phase 1
NCT01481129 National Cancer Institute (NCI) Diffuse Large B Cell Lymphoma December 2011 Phase 2
NCT01071018 Merck Sharp & Dohme Corp. Solid Tumors February 2010 Phase 1
NCT01319539 National Cancer Institute (NCI) Estrogen Receptor Negative|Estrogen Receptor Positive|HER2+Neu Negative|HER2+Neu Positive|Progesterone Receptor Negative|Progesterone Receptor Positive|Stage IA Breast Cancer|Stage IB Breast Cancer|Stage IIA Breast Cancer|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Triple-Negative Breast Carcinoma April 2011 Phase 2
NCT01263145 National Cancer Institute (NCI) Adult Solid Neoplasm|Recurrent Breast Carcinoma|Stage IV Breast Cancer January 5, 2011 Phase 1
NCT01344031 National Cancer Institute (NCI) Estrogen Receptor Positive|Invasive Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer AJCC v6 and v7 April 21, 2011 Phase 1
NCT01802320 National Cancer Institute (NCI) Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Rectal Mucinous Adenocarcinoma|Rectal Signet Ring Cell Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer March 2013 Phase 2
NCT01802320 National Cancer Institute (NCI) Colon Mucinous Adenocarcinoma|Colon Signet Ring Cell Adenocarcinoma|Rectal Mucinous Adenocarcinoma|Rectal Signet Ring Cell Adenocarcinoma|Recurrent Colon Carcinoma|Recurrent Rectal Carcinoma|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer March 2013 Phase 2
NCT01147211 National Taiwan University Hospital Non Small Cell Lung Cancer September 2010 Phase 1
NCT01260701 National Cancer Institute (NCI) Adenocarcinoma of the Gastroesophageal Junction|Diffuse Gastric Adenocarcinoma|Gastric Intestinal Type Adenocarcinoma|Gastric Mixed Adenocarcinoma|Recurrent Gastric Carcinoma January 2011 Phase 2
NCT01169649 Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp. PANCREAS|Neuroendocrine July 2010 Phase 2
NCT01253447 National Cancer Institute (NCI) Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia October 2010 Phase 2
NCT01295632 Merck Sharp & Dohme Corp. Advanced Cancer February 2011 Phase 1
NCT01245205 National Cancer Institute (NCI) HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Unspecified Adult Solid Tumor, Protocol Specific November 2010 Phase 1
NCT01481129 National Cancer Institute (NCI) Diffuse Large B Cell Lymphoma December 2011 Phase 2
NCT01283035 National Cancer Institute (NCI) Ovarian Sarcoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma April 2011 Phase 2
NCT01281163 National Cancer Institute (NCI) Estrogen Receptor Negative|Estrogen Receptor Positive|HER2+Neu Positive|Progesterone Receptor Negative|Progesterone Receptor Positive|Recurrent Breast Carcinoma|Stage IV Breast Cancer January 2011 Phase 1
NCT01249105 Dana-Farber Cancer Institute|Brigham and Women´s Hospital|Massachusetts General Hospital|Beth Israel Deaconess Medical Center|Memorial Sloan Kettering Cancer Center|University of California, Los Angeles|Merck Sharp & Dohme Corp. Malignant Glioma Phase 2
NCT01344031 National Cancer Institute (NCI) Estrogen Receptor Positive|Invasive Breast Carcinoma|Recurrent Breast Carcinoma|Stage IV Breast Cancer AJCC v6 and v7 April 21, 2011 Phase 1
NCT00963547 Merck Sharp & Dohme Corp. Advanced Solid Tumors|Breast Cancer September 15, 2009 Phase 1
NCT01466868 Centre Leon Berard|National Cancer Institute, France Diffuse Large B Cell Lymphoma November 2011 Phase 2
NCT01307631 National Cancer Institute (NCI) Endometrial Adenocarcinoma|Endometrial Adenosquamous Carcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Serous Adenocarcinoma|Recurrent Uterine Corpus Carcinoma March 2011 Phase 2
NCT01235897 University of California, San Francisco|Merck Sharp & Dohme Corp. Advanced Solid Tumors|Tumors|Cancer March 2011 Phase 1
NCT01294306 National Cancer Institute (NCI) Adenosquamous Lung Carcinoma|Bronchioloalveolar Carcinoma|Large Cell Lung Carcinoma|Lung Adenocarcinoma|Recurrent Non-Small Cell Lung Carcinoma|Squamous Cell Lung Carcinoma February 2011 Phase 2
Solvent & Solubility
In Vitro: 

DMSO : 4.9 mg/mL (10.20 mM; Need ultrasonic and warming)

H2O : 3.81 mg/mL (7.93 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
ConcentrationSolventMass 1 mg 5 mg 10 mg
1 mM 2.0816 mL 10.4082 mL 20.8164 mL
5 mM 0.4163 mL 2.0816 mL 4.1633 mL
10 mM 0.2082 mL 1.0408 mL 2.0816 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    MK 2206 is prepared in vehicle (30% captisol).

  • 2.

    MK 2206 dihydrochloride is prepared in Vehicle (corn oil+5% DMSO).


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