VER-49009

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

VER-49009 是一种有效的 HSP90 抑制剂（IC50 =25 nM，Kd=78 nM）。

VER-49009 is a potent HSP90 inhibitor. VER-49009 inhibits Hsp90 with an IC50 value of 47 nM. VER-49009 produces a cellular antiproliferative GI50 value of 685 nM when tested against a human cancer cell line panel. Consistent with inhibition of Hsp90, VER-49009 induces the expression of Hsp27 and Hsp72 while reducing the client proteins C-RAF, B-RAF, survivin, and PRMT5, causing cell cycle arrest and apoptosis.

VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM. VER-49009 binds to the ATPase of full length yeast Hsp90 protein, with an IC50 of 140 nM. VER-49009 inhibits Hsp90, with a Kd of 78 nM. VER-49009 also shows antiproliferative activities against various human cancer cells, with a mean GI50 of 685 ± 119 nM. VER-49009 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 values of 444 ± 91.1 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. VER-49009 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-49009 inhibits the proliferation (1, 2.5 μM), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 μM).

VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with client protein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors.

VER49009 | VER 49009 | VER-49009

Metabolic Enzyme/Protease

Factor Xa

HSP90β

Cancer

——

558640-51-0

387.82

C19H18ClN3O4

>98% (HPLC)

DMSO : 100 mg/mL 257.85 mM;H2O : < 0.1 mg/mL

c1(c(cc(c(c1)c1c(c([nH]n1)C(=O)NCC)c1ccc(cc1)OC)O)O)Cl

3-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years