Cabozantinib (XL184, BMS-907351) , ≥98% , 849217-68-1

CAS NO.：849217-68-1

Empirical Formula: C28H24FN3O5

Molecular Weight: 501.51

MDL number: MFCD20926324

EINECS: 692-846-8

PRODUCT Properties

• Melting point: 212-215°C
• Boiling point: 758.1±60.0 °C(Predicted)
• Density: 1.396
• storage temp.: -20°C
• solubility: Soluble in DMSO
• form: White powder.
• pka: 13.86±0.70(Predicted)
• color: White
• 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.
• InChIKey: ONIQOQHATWINJY-UHFFFAOYSA-N
• SMILES: C1(C(NC2=CC=C(OC3C4C(N=CC=3)=CC(OC)=C(OC)C=4)C=C2)=O)(C(NC2=CC=C(F)C=C2)=O)CC1

Description and Uses

Cabozantinib was approved inNovember 2012 for the treatment of patients with progressive, unresectable, locally advanced, or metastatic medullary thyroid cancer (MTC). Cabozantinib was granted orphan drug status by the FDA to facilitate development of newtreatment options for patients with MTC. It is a member of a class of tyrosine kinase inhibitors (TKIs) with nanomolar pan-inhibitory activity against VEGFR2, MET, and RET among others. Inhibition of the VEGF pathway has been shown preclinically to initially slow tumor growth, but rapid revascularization is followed by aggressive tumor growth. The MET pathway has been implicated in the development of VEGF resistance, so dual VEGF/MET activity is viewed as desirable. In addition, mutations in RET play a particular role in MTC, with 25% of the tumors inheriting a germlinemutation in the proto-oncogene, so multiple tyrosine kinase inhibition may be viewed as particularly beneficial for the treatment of MTC.

XL184 can be used in biological study. Computational network biological approach based on pathway cross-talk inhibition identified new synergistic drug combinations using raloxifene and cabozantinib for treatment of human breast cancer in xenograft mouse model. Potent c-MET inhibitor.

Safety

• Symbol(GHS): GHS05
• Signal word: Danger
• Hazard statements: H315-H318
• Precautionary statements: P264-P280-P302+P352-P321-P332+P313-P362-P280-P305+P351+P338-P310