CAS:1173111-67-5PF-04929113 Mesylate

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Synonyms: SNX-5422 Mesylate

PF-04929113 mesylate is a potent and selective Hsp90 inhibitor with an IC50 of median 50 nM.

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18817579266

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18817579266

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实验数据

技术信息

生物活性

靶点 HSP90

IC50:50nM
描述HSP90 (heat shock protein 90) is a cellular ubiquitous molecular chaperone responsible for promoting the conformational mutation and stabilization of several client oncoproteins, including Met, B-Raf, p53, Akt, and Kit, function of which is required by tumor cells to maintain appropriate client protein expression necessary for proliferation and survival. PF-04929113 is prodrug form of HSP90 inhibitor SNX-2112 and perform similarly as SNX-2112 on client protein of HSP90, such as induction of Hsp70 (in A375 cells) and decrease of Her2 (in AU565 cells) with IC50 values of 13nM and 5nM, respectively. PF-04929113 was orally bioavailable and efficacious in various xenograft tumor models, such as dose-dependent tumor growth inhibition by oral dosing of 10-50mg/kg PF-04929113 in HT-29 colon tumor xenograft model^[1].
动物研究
剂量
Mice^[1] (p.o.): 5 mg/kg - 50 mg/kg

给药途径
p..o.

动物药代数据
Animal Mice^[1]
Dose 25 mg/kg
Administration p.o.
AUC_0→inf 11004 h·ng/ml
T_1/2 2.9 h
T_max 1 h
C_max 2148 ng/ml