SNX 2112

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SNX 2112 (PF 04928473) 是一种有效的选择性 Hsp90 抑制剂，对 HSP90α 和 HSP90β 的结合 IC50 均为 30 nM。

SNX 2112 (PF 04928473) is a potent, selective Hsp90 inhibitor with binding IC50 of 30 nM for both HSP90α and HSP90β; shows weak affinity for Hsp90 family members Grp94 and Trap-1 (IC50=0.8-4.2 uM); has properties and potency, including degradation of HER2, mutant EGFR, and other client proteins, inhibition of ERK and Akt activation, and induction of a Rb-dependent G1 arrest with subsequent apoptosis; the orally bioavailbe prodrug SNX-5422, inhibits MM cell growth and prolongs survival in a xenograft murine model.

SNX-2112 is an orally active Hsp90 inhibitor, with a Kd 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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PF 04928473

Cytoskeleton/Cell Adhesion Molecules

HSP

HSP90α|HSP90β

Cancer

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908112-43-6

464.489

C23H27F3N4O3

>98% (HPLC)

DMSO: 86 mg/mL (185.2 mM); Ethanol: 1 mg/mL (2.15 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(N)C1=CC=C(N2N=C(C(F)(F)F)C3=C2CC(C)(C)CC3=O)C=C1N[C@H]4CC[C@H](O)CC4

4-(6,6-Dimethyl-4-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-indazol-1-yl)-2-(trans-4-hydroxy-cyclohexylamino)-benzamide

(-20℃)

With Ice Pack

≥ 2 years