Temsirolimus

Rapamycin (Cay-13346) is an immunosuppressant that specifically interacts with the cytosolic FK-binding protein 12 to form a complex which inhibits the mammalian target of rapamycin (mTOR) pathway by directly binding to mTOR Complex 1. Temsirolimus is a dihydroxymethyl propionic acid ester of rapamycin with improved solubility that specifically inhibits mTOR signaling with a potency similar to that of rapamycin. Treatment with temsirolimus leads to cell cycle arrest in the G1 phase and also inhibition of tumor angiogenesis by reducing synthesis of VEGF. Temsirolimus demonstrates cytostatic activity in several xenograft models of human tumors in nude mice, including glioblastomas, prostate carcinoma, pancreatic, liver, and breast cancers, and medulloblastoma.Formal Name: 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate] rapamycin. CAS Number: 162635-04-3. Synonyms: CCI-779, Torisel(R). Molecular Formula: C56H87NO16. Formula Weight: 1030.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.20 mg/ml, DMSO: 12.5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 268, 277, 289 nm. SMILES: O=C(O[C@](CC([C@H](C)/C=C(C)/[C@@H](O)[C@@H](OC)C([C@@H](C1)C)=O)=O)([H])[C@H](C)C[C@@H]2CC[C@@H](OC(C(C)(CO)CO)=O)[C@H](OC)C2)[C@@]3([H])N(C(C([C@@]4(O)[C@H](C)CC[C@](C[C@@H](/C(C)=C/C=C/C=C\[C@H]1C)OC)([H])O4)=O)=O)CCCC3. InChi Code: InChI=1S/C56H87NO16/c1-33-17-13-12-14-18-34(2)45(68-9)29-41-22-20-39(7)56(67,73-41)51(63)52(64)57-24-16-15-19-42(57)53(65)71-46(30-43(60)35(3)26-38(6)49(62)50(70-11)48(61)37(5)25-33)36(4)27-40-21-23-44(47(28-40)69-10)72-54(66)55(8,31-58)32-59/h12-14,. InChi Key: CBPNZQVSJQDFBE-PXVOFZQNSA-N.