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SML3915

Sigma-Aldrich

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

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About This Item

Empirical Formula (Hill Notation):
C28H24FN3O5·C4H6O5
CAS Number:
Molecular Weight:
635.59
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

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

Pictograms

Health hazardCorrosion

Signal Word

Danger

Hazard Statements

Hazard Classifications

Eye Dam. 1 - Repr. 1B - Skin Irrit. 2 - STOT RE 2

Target Organs

Bone marrow,Kidney,Endocrine system,Gastrointestinal tract,Liver

WGK

WGK 3

Regulatory Information

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Certificates of Analysis (COA)

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Cabozantinib: A Multitargeted Oral Tyrosine Kinase Inhibitor
Pharmacotherapy, 38(3), 357-369 (2018)
Cabozantinib Enhances Anti-PD1 Activity and Elicits a Neutrophil-Based Immune Response in Hepatocellular Carcinoma
Clinical Cancer Research, 28(11), 2449-2460 (2022)
F Michael Yakes et al.
Molecular cancer therapeutics, 10(12), 2298-2308 (2011-09-20)
The signaling pathway of the receptor tyrosine kinase MET and its ligand hepatocyte growth factor (HGF) is important for cell growth, survival, and motility and is functionally linked to the signaling pathway of VEGF, which is widely recognized as a

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