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CC-671

CC-671

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商品描述
CC-671,HY-108709,MCE:
Description

CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.

IC50 & Target

Clk2

0.006 μM (IC50)

In Vitro

CC-671 (compound 23) is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively. HCT-116 cell lysates treated with CC-671 at 3 μM for 1 h demonstrates that only four kinases show cellular binding of 75% or more including CLK2, CAMKK2, PIP4K22, and JNK.

In Vivo

CC-671 (compound 23) demonstrates significant tumor growth inhibition (TGI) ((vehicle -treated/vehicle) ×100%) of 71% at both 10 and 20 mg/kg on a every 3 days (q3d) dosing schedule. The body weight loss (BWL) in the CC-671 treated group (20 mg/kg ) is higher than in the 10 mg/kg group (17% vs 5%).

Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (117.06 mM)

H2O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9510 mL 9.7550 mL 19.5099 mL
5 mM 0.3902 mL 1.9510 mL 3.9020 mL
10 mM 0.1951 mL 0.9755 mL 1.9510 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.06 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.08 mg/mL (4.06 mM); Clear solution; Need warming

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.06 mM); Suspended solution; Need ultrasonic


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