SML3915

Cabozantinib malate

≥98% (HPLC)

• Synonym(s): BMS 907351 (S)-malate, BMS-907351 (S)-malate, BMS907351 (S)-malate, Cabozantinib (L)-malate, Cabozantinib (S)-malate, N-(4-(6,7-Dimethoxyquinolin-4-yloxy)phenyl)-N’-(4-fluorophenyl)cyclopropane1,1-dicarboxamide, (2S)-hydroxybutanedioate, N-(4-{[6,7-bis(Methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (L)-malate salt, XL 184 (S)-malate, XL-184 (S)-malate, XL184 (S)-malate
• Empirical Formula (Hill Notation): C₂₈H₂₄FN₃O₅·C₄H₆O₅
• CAS Number: 1140909-48-3
• Molecular Weight: 635.59
• MDL number: MFCD20923480
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Description

Biochem/physiol Actions

Orally active, potent receptor tyrosine kinase inhibitor against VEGFR2 (KDR), MET, KIT, RET, AXL, TIE2, and FLT3 with anti-tumor efficacy in vivo.


Cabozantinib (XL184; BMS‐907351) is an orally active, potent inhibitor against multiple receptor tyrosine kinases, notably VEGFR2/KDR (IC50 = 35 pM), MET (IC50 = 1.3 nM/wt, 3.8 nM/Y1248H, 11.8 nM/D1246N, 14.6 nM/K1262R), KIT, RET, AXL, TIE2, and FLT3 (IC50 = 4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib inhibits MET-driven proliferation in cancer cultures (IC50 = 9.9 nM/Hs746T, 19 nM/SNU-5) and simultaneously suppressing metastasis, angiogenesis and tumor growth in vivo (3-100 mg/kg via single or daily p.o. to mice with human MDA-MB-231 xenograft, 1-60 mg/kg via single or daily p.o. to rats with C6 rat glioma).

Caution

Hygroscopic