NVP-BEP800

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

一种有效的选择性 Hsp90β 抑制剂，IC50 为 58 nM；对 Grp94 和 Trap-1 显示 >70 倍的选择性。

A potent and selective Hsp90β inhibitor with IC50 of 58 nM; shows >70-fold selective against Grp94 and Trap-1; induces ErbB2, B-Raf(V600E), Raf-1, Akt and Hsp70 induction in A375 melanoma and BT-474 breast cancer cell lines; orally bioactive.Breast Cancer Preclinical.

VER-82576 (NVP-BEP800) is a potent and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β and is >70-fold selective against Grp94 and Trap-1, with IC50s of 4.1 ± 1.1 and 5.5 ± 0.48 μM. VER-82576 potently inhibits the proliferation of tumor cells, with GI50s ranging from 38 nM in A375 cells to 1050 nM in PC3 cells, with an average GI50 of 245 nM. VER-82576 (250-1250 nM) depletes client proteins in human cancer cell lines in vitro. VER-82576 (NVP-BEP800; 200 nM) shows no significant effect on the ionizing radiation (IR) dose-response curves of A549 cells, and is less toxic to SNB19 cells. VER-82576 in combination with IR results in more severe DNA damage in both A549 and SNB19 cell lines than each treatment alone and also protracts the kinetics of DNA damage repair in SNB19 cells. VER-82576 (NVP-BEP800; 0.05, 0.1 or 0.2 μM) dose-dependently decreases the viability and induces apoptosis of glioblastoma cells. VER-82576 (0.2 μM) suppresses the expression of IKKβ protein but does not alter the levels of IKKβ mRNA in T98G cells. VER-82576 (0.2 μM) suppresses the expression of heat shock protein 70.

VER-82576 (NVP-BEP800; 15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice.

VER-82576 | VER82576

Cytoskeleton/Cell Adhesion Molecules

HSP

HSP90β

Cancer

Breast Cancer

847559-80-2

480.4106

C21H23Cl2N5O2S

>98% (HPLC)

DMSO: 6.2 mg/mL (Need ultrasonic)

O=C(C1=CC2=C(C3=CC(OCCN4CCCC4)=C(Cl)C=C3Cl)N=C(N)N=C2S1)NCC

Thieno[2,3-d]pyrimidine-6-carboxamide, 2-amino-4-[2,4-dichloro-5-[2-(1-pyrrolidinyl)ethoxy]phenyl]-N-ethyl-

(-20℃)

With Ice Pack

≥ 2 years