VER-49009 是一种有效的 HSP90 抑制剂,IC50值为 25 nM,Kd值为 78 nM。
产品描述
VER-49009 is a potent Hsp90 inhibitor(IC50 of 25 nM and Kd of 78 nM).
体外活性
VER-49009 inhibited the proliferation of hepatic stellate cell line CFSC cells, and both of them induced G2 phase arrest in CFSC cells[1].
体内活性
Treatmented with VER-49009 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[2].
激酶实验
Fluorescence Polarization Assay: Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.
细胞实验
Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method. (Only for Reference)
Cas No.
558640-51-0
分子式
C19H18ClN3O4
分子量
387.82
别名
CCT 129397
储存和溶解度
DMSO:100 mg/mL (257.85 mM),Need ultrasonic
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years