PF-04929113

PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04928473 (SNX-2112, Cay-22359), which binds both Hsp90alpha and Hsp90beta with an IC50 value of 30 nM. The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration. The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells. Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.Formal Name: glycine, trans-4-[[2-(aminocarbonyl)-5-[4,5,6,7-tetrahydro-6,6-dimethyl-4-oxo-3-(trifluoromethyl)-1H-indazol-1-yl]phenyl]amino]cyclohexyl ester. CAS Number: 908115-27-5. Synonyms: SNX-5422. Molecular Formula: C25H30F3N5O4. Formula Weight: 521.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.25 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 250, 359 nm. SMILES: O=C(CN)O[C@@H](CC1)CC[C@H]1NC2=CC(N3N=C(C(F)(F)F)C4=C3CC(C)(C)CC4=O)=CC=C2C(N)=O. InChi Code: InChI=1S/C25H30F3N5O4/c1-24(2)10-18-21(19(34)11-24)22(25(26,27)28)32-33(18)14-5-8-16(23(30)36)17(9-14)31-13-3-6-15(7-4-13)37-20(35)12-29/h5,8-9,13,15,31H,3-4,6-7,10-12,29H2,1-2H3,(H2,30,36)/t13-,15-. InChi Key: AVDSOVJPJZVBTC-CTYIDZIISA-N.