Deforolimus

A potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; displays significant antiproliferative activity a broad panel of cell lines with EC50 of 0.2-2.3 nM; potently and selectively inhibits VEGF production in a dose-dependent manner; exerts significant antitumor effects in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas) or A549 (lung) xenografts.Breast Cancer Phase 2 Clinical (In Vitro) :Treatment of HT-1080 fibrosarcoma cells with Ridaforolimus results in a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50s of 0.2 and 5.6 nM, respectively, and EC50s of 0.2 and 1.0 nM, respectively. In HT-1080 cells, the EC50 for inhibition of cell proliferation (0.5 nM) is similar to the EC50s for inhibition of S6 and 4E-BP1 phosphorylation. Exposure to Ridaforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of Ridaforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Ridaforolimus exhibits a predominantly cytostatic mode of action, consistent with the findings for other mTOR inhibitors. Potent inhibitory effects on vascular endothelial growth factor secretion, endothelial cell growth, and glucose metabolism. (In Vivo) :Ridaforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Ridaforolimus inhibits tumor growth in a dose-dependent manner, with 0.3 mg/kg being the lowest dose that inhibits tumor growth significantly and 3 and 10 mg/kg doses achieving maximum inhibition.

572924-54-0

AP-23573 | MK-8669 | Ridaforolimus

>98% (HPLC)

DMSO: ≥ 44 mg/mL

[H][C@@]12CC[C@@H] (C) [C@@] (O) (O1) C (=O) C (=O) N1CCCC[C@@]1 ([H]) C (=O) O[C@@H] (CC (=O) [C@H] (C) \C=C (C) \[C@@H] (O) [C@@H] (OC) C (=O) [C@H] (C) C[C@H] (C) \C=C\C=C\C=C (C) \[C@H] (C2) OC) [C@H] (C) C[C@@H]1CC[C@@H] (OP (C) (C) =O) [C@@H] (C1) OC |r, c:31,50, t:46,48|

C53H84NO14P

990.2061

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.