SNX-2112,908112-43-6

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SNX-2112

CAS No. : 908112-43-6

MCE 国际站：SNX-2112

产品活性：SNX-2112 (PF 04928473) 是一种可口服的 Hsp90 抑制剂，K_d 值为 16 nM，对 Hsp90 α 和 Hsp90β 的 IC₅₀ 值均为 30 nM；同时可诱导 Her-2 的降解, 抑制 Grp94 和 Trap-1 的活性， IC₅₀ 值分别为 10 nM，4.275 μM 和 0.862 μM。SNX-2112 (PF 04928473) 结合 Hsp90 亚型 Hsp90α, Hsp90β 和 Hsp90b1/Grp94，K_d 分别为 4 nM, 6 nM 和 484 nM。

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

作用靶点：HSP  |  Autophagy

In Vitro: SNX-2112 is an orally active Hsp90 inhibitor, with a K_d of 16 nM, and also induces Her-2 degradation, with an IC₅₀ of 10 nM. SNX-2112 binds to Hsp90, with IC₅₀s of 30 nM, 30 nM, 4.275 μM and 0.862 μM for Hsp90 α and β, Grp94 and Trap-1, respectively. SNX-2112 shows potent antiproliferative activity against various cancer cell types, with IC₅₀s of 3 nM to 53 nM. SNX-2112 exhibits potent effects on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells, with IC₅₀s of 11 ± 5, 41 ± 12, and 1 ± 0.6 nM, respectively. SNX-2112 also induces Hsp70 in A375 cells with an IC₅₀ of 2 ± 0.9 nM. In addition, SNX-2112 potently blocks signaling of Hsp90 clients, such as Akt, ERK, and NF-κB pathways in different cells. SNX-2112 inhibits multiple myeloma (MM) cell growth, including MM.1S, U266, INA-6, RPMI8226, OPM1, OPM2, MM.1R, and Dox40 MM cell lines, with IC₅₀s of 52, 55, 19, 186, 89, 67, 93, and 53 nM at 48 hours, respectively. SNX-2112 (2.5-10 nM) also suppresses osteoclast formation, associated with down-regulation of ERK/c-fos and PU.1.

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