VER-82576 (NVP-BEP800) 是一种有效的，可口服的，选择性的 Hsp90 抑制剂，对 Hsp90β 的 IC₅₀ 值为 58 nM；VER-82576 同时可较弱地抑制 Grp94 和 Trap-1 的活性，IC₅₀ 值分别为 4.1 和 5.5 μM。

VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC 50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC 50 s of 4.1 and 5.5 μM, respectively.

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HSP90β 58 nM (IC50) GRP94 4.1 μM (IC5

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)

VER-82576 (NVP-BEP800; 15 or 30 mg/kg, p.o.) shows antitumor activities in A375 cancer xenografts and BT-474 xenograft-bearing mice. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Massey AJ, et al. Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800. Mol Cancer Ther. 2010 Apr;9(4):906-19.
[2]. Niewidok N, et al. Hsp90 Inhibitors NVP-AUY922 and NVP-BEP800 May Exert a Significant Radiosensitization on Tumor Cells along with a Cell Type-Specific Cytotoxicity. Transl Oncol. 2012 Oct;5(5):356-69. Epub 2012 Oct 1.

In Vitro: DMSO : 6.2 mg/mL (12.91 mM; Need ultrasonic)配制储备液