Cabozantinib

Cabozantinib is a potent multi-targeted receptor tyrosine kinase (RTK) inhibitor of endothelial growth factor receptor 2 (VEGFR2) (IC50=0.035nM), the hepatocyte growth factor receptor c-Met (IC50=1.3nM), AXL (IC50=7nM), fms like tyrosine kinase 3 (FLT3) (IC50=11.3nM), mast/stem cell growth factor (KIT) (IC50=4.6nM), RET (IC50=5.2nM), tyrosine-protein kinase receptor (TIE-2) (IC50=14.3nM) and RON (IC50=124nM). Cabozantinib reduces cell proliferation and vascular density. It also induces apoptosis and intratumoral hypoxia. Cabozantinib exhibits dose-related tumor growth inhibition, tumor regression, angiogenesis and/or metastasis inhibition in a broad range of preclinical tumor models. The anticancer compound cabozantinib has undergone clinical trial in a broad number of cancers, including thyroid carcinoma, prostate cancer, ovarian cancer, melanoma, breast cancer, non-small cell lung cancer, hepatocellular cancer, renal cell carcinoma and glioblastoma. Product References: (1) Y. Zhang, et al., IDrugs 13, 112 (2010) , (2) R. Kurzrock, et al., J. Clin. Oncol. 29, 2660 (2011) , (3) F.M. Yakes, et al., Mol. Canc. Ther. 10, 2298 (2011) , (4) S. Roy, et al., Anticancer Agents Med. Chem. 15, 37 (2015) (Review) , (5) N.M. Tannir, et al., Curr. Oncol. Rep. 19, 14 (2017) (Review) , (6) C. Grullich, Recent Res. Cancer Res. 211, 67 (2018) (Review) , (7) J.N. Markowitz & K.M. Fancher,, Pharmacotherapy 38, 357 (2018) (Review) , (8) A. Desai & E.J. Small, Future Oncol. 15, 2337 (2019) (Review) , (9) J. Trojan, Drugs 80, 1203 (2020) (Review) Appearance: White to off-white solid. Solubility: Soluble in DMSO (20mg/ml). Slightly soluble in ethanol. Identity: Determined by 1H-NMR. InChi Key: ONIQOQHATWINJY-UHFFFAOYSA-N Smiles: O=C(NC1=CC=C(OC2=C3C=C(C(OC)=CC3=NC=C2)OC)C=C1)C4(C(NC5=CC=C(C=C5)F)=O)CC4