VER-50589

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-50589 是一种有效的 HSP90 抑制剂。

VER-50589 is a potent Hsp90 inhibitor. VER-50589 inhibits Hsp90 with an IC50 value of 21 nM. It produces a mean cellular antiproliferative GI50 value of 78 nM when tested against a human cancer cell line panel. VER-50589 shows favorable pharmacokinetics and impairs tumor growth in animals.

VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM. VER-50589 inhibits intrinsic ATPase of full-length recombinant yeast Hsp90, with an IC50 of 143 ± 23 nM in the presence of 400 μM ATP. VER-50589 shows antiproliferative activities against various human cancer cells, with the lowest GI50 of 32.7 ± 0.2 nM for CH1 human ovarian cells, and mean GI50 of 78 ± 15 nM. VER-50589 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 value of 19 ± 2.4 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. Furthermore, VER-50589 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-50589 also causes G1 and G2-M block (115 or 575 nM) and induces cytostasis in HCT116 colon cancer cells. In addition, VER-50589 causes great uptake in HCT116 cells.

VER-50589 (4 mg/kg, i.p.) exerts a complete HSP90 inhibition in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors. VER-50589 (100 mg/kg, i.p.) shows reduced tumor volume and tumor weights in the HCT116 colon carcinoma xenografts compared to the control mice group.

VER50589 | VER 50589 | VER-50589

Apoptosis

NF-κB

HSP90β

Cancer

——

747413-08-7

388.8

C19H17ClN2O5

>98% (HPLC)

DMSO : ≥ 48 mg/mL; 123.46 mM

c1(cc(c(cc1O)O)c1c(c2ccc(cc2)OC)c(no1)C(=O)NCC)Cl

5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)isoxazole-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years