SNX-5422,1173111-67-5

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SNX-5422 Mesylate

CAS No. : 1173111-67-5

MCE 国际站：SNX-5422 Mesylate

产品活性：SNX-5422 Mesylate (PF-04929113 Mesylate) 是 SNX-2112 的前体药物，为可口服的 Hsp90 抑制剂，K_d 值为 41 nM，同时可诱导 Her-2 的降解，IC₅₀ 值为 37 nM。

研究领域：Cell Cycle/DNA Damage | Metabolic Enzyme/Protease

作用靶点：HSP

In Vitro: SNX-5422 is an orally active Hsp90 inhibitor, with a K_d of 41 nM, and also induces Her-2 degradation, with an IC₅₀ of 37 nM. SNX-5422 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC₅₀s of 5 ± 1, 11 ± 3, and 61 ± 22 nM, respectively. SNX-5422 also induces Hsp70 in A375 cells with an IC₅₀ of 13 ± 3 nM. SNX-5422 (SNX5422; 0.5, 1, 2, 5, and 10 μM) reduces cell viability in a concentration-dependent manner. Moreover, SNX-5422 (1, 3, 5, 7 μM) in combination with equal amounts of HDAC inhibitors (PXD101, SAHA, and TSA) synergistically induces cell death via suppression of PI3K/Akt/mTOR signaling in ATC cells.

In Vivo: SNX-5422 (50 mg/kg, p.o.) efficiently inhibits tumor growth of HT-29 human colon tumor xenograft model after administration 3 times a week for 3 weeks (qod × 3/2 × 3). SNX-5422 (20, 40 mg/kg, p.o.) markedly inhibits multiple myeloma (MM) tumor growth and angiogenesis in mice.

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