Sirolimus Rapamycin MTOR Inhibitors

Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. [1] In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR.

Properties:

Appearance & Physical State: yellow solid

Density: 1.182 g/cm3

Boiling Point: 973.017ºC at 760 mmHg

Melting Point: 183-185ºC

Flash Point: 542.261ºC

Refractive Index: 1.55

Stability: Stable if stored as directed.

Related Products:

Everolimus; Temsirolimus; PI-103; Torin 1; PF-04691502; Apitolisib; Torin 2; BGT226; Palomid 529; Deforolimus; KU-0063794; Tacrolimus

[1] Edwards SR, et al. J Biol Chem, 2007, 282(18), 13395-13401.

[2] Barbet NC, et al. Mol Biol Cell, 1996, 7(1), 25-42.