VER49009 是一种有效的 HSP90 抑制剂（IC50 =25 nM，Kd=78 nM）。
产品描述
VER-49009 is an effective HSP90 inhibitor(IC50 =25 nM, Kd=78 nM).
体外活性
在人卵巢肿瘤模型中,腹腔注射VER-49009（4 mg/kg）能够诱导HSP90与ERBB2的解离.在无胸腺的小鼠中,静脉注射VER-49009（20 mg/kg ）能够发挥有效作用.
体内活性
VER-49009能够诱导HSP72和HSP27与与其结合蛋白解离,导致细胞周期停滞。在重组的酵母Hsp90蛋白中（IC50=167 nM）,VER-49009能够抑制內源性ATP酶活性。在肝纤维化的治疗中,VER-49009能够诱导肝细胞CFSC在G2期停滞积累,抑制细胞生长。
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.
940289-57-6
分子式
C19H18ClN3O4
分子量
387.82
别名
CCT0129397;VER-49009;VER 49009
储存和溶解度
DMSO:71 mg/mL (183.1 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
