Cabozantinib (849217-68-1) is a novel inhibitor of c-met and VEGFR2 kinase activity, IC50=3.5 nm and 35 pM respectively.1 Inhibits MET-activating kinase domain mutations Y1248H, D1246N or K1262R, IC50=3.8, 11.8 and 14.6 nM respectively. In cellular assays it inhibits the following kinases: MET, VEGF2, KIT, FLT3 and AXL, IC50=7.8, 1.9, 5.0, 7.5 and 42 μM respectively.1 Eliminated approximately 80% of vasculature in spontaneous pancreatic islet tumors over 7 days in a mouse model.2 Clinically useful anticancer agent.3 Met和VEGFR2抑制剂cabozantinib(849213 -68-1)是一种新的抑制c-met和VEGFR2激酶活性的抑制剂,IC50分别为3.5 nm和35 pM 抑制met激活激酶结构域突变Y1248H, D1246N或K1262R, IC50分别为3.8,11.8和14.6 nM。 在细胞实验中,它对MET、VEGF2、KIT、FLT3和AXL有抑制作用,IC50分别为7.8、1.9、5.0、7.5和42 μM 在小鼠模型中,在7天内消除自发性胰岛肿瘤中约80%的血管 临床上有用的抗癌剂。
References/Citations:
1) Yakes et al. (2011), Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth; Mol. Cancer Ther., 10 2298 2) You et al. (2011), VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer; Cancer Res., 71 4758 3) Kurzrock et al. (2011), Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor in patients with medullary thyroid cancer; J. Clin. Oncol., 29 2660
CAS:
849217-68-1
Catalog Number:
10-3231
Activity:
Met and VEGFR2 inhibitor
Chemical Name:
N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Alternate Names:
XL-184; BMS-907351; Carbozantinib
Molecular Weight:
501.51
Molecular Formula:
C28H24FN3O5 Solubility:
Soluble in DMSO
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
更多产品咨询联系 上海惠诚生物科技有限公司 联系人:任经理 电话:18017273415