Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator.

Rapamycin (12.5 nM, 25 nM, 50 nM, 100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM. 
Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2.

Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group.

DMSO : 150 mg/mL (164.08 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

• 1.

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

  Solubility: ≥ 2.5 mg/mL (2.73 mM); Clear solution

• 2.

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

  Solubility: 2.5 mg/mL (2.73 mM); Suspended solution; Need ultrasonic and warming

• 3.

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

  Solubility: ≥ 2.5 mg/mL (2.73 mM); Clear solution