VER-82576
Cat. No.:YN370457
CAS No. :847559-80-2
产品名称: | VER-82576 |
CAS No.: | 847559-80-2 |
Chemical Name: | 2-amino-4-[2,4-dichloro-5-[2-(1-pyrrolidinyl)ethoxy]phenyl]-N-ethyl-thieno[2,3-d]pyrimidine-6-carboxamide |
Synonyms: | NVP-BEP800 |
分子量: | 480.41 |
分子式: | C₂₁H₂₃Cl₂N₅O₂S |
SMILES: | O=C(C1=CC2=C(N=C(N=C2S1)N)C3=CC(OCCN4CCCC4)=C(C=C3Cl)Cl)NCC |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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。 |
IC50和靶点: | [{name:"HSP90β:58 nM (IC50)"},{name: "GRP94:4.1 μM (IC50)"},{name: "TRAP-1:5.5 μM (IC50)"}] |
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Massey, A.J., Schoepfer, J., Brough, P.A., et al.Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800Mol. Cancer Ther.9(4),906-919(2010)
Wu, J., Wang, W., Shao, Q., et al.Irradiation facilitates the inhibitory effect of the heat shock protein 90 inhibitor NVP-BEP800 on the proliferation of malignant glioblastoma cells through attenuation of the upregulation of heat shock protein 70Exp. Ther. Med.8(3),893-898(2014)
Chen, W., Sin, S.H., Wen, K.W., et al.Hsp90 inhibitors are efficacious against Kaposi Sarcoma by enhancing the degradation of the essential viral gene LANA, of the viral co-receptor EphA2 as well as other client proteinsPLoS Pathog.8,(2012)