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XL184 (Cabozanitinib) | VEGFR2/MET inhibitor

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Price:
$109.00
Catalog #:
C9518-5
Quantity:


Product Description

XL184 (Cabozantinib) is an oral, small-molecule inhibitor, which has potent activity toward VEGFR2 (IC50=0.035nM) and MET (IC50 = 1.3nM), as well as a number of other receptor tyrosine kinases that have also been implicated in tumor pathobiology, including RET, KIT, AXL, and FLT3 [1].

Multiple receptor tyrosine kinases (RTKs) are sometimes activated in the same tumor. Inhibition of single RTK may lead to compensatory signaling that maintains cell growth. Targeting multiple kinases simultaneously might overcome both intrinsic and acquired resistance to antitumor drugs. XL184 has been shown to inhibit phosphorylation of MET and VEGFR2, to disrupt angiogenesis and cellular migration and invasion, and to promote tumor and endothelia cell death1. Inhibition of c-Met with XL184 blocks self-renewal capacity in pancreatic cancer stem cells (CSCs) [2]. In mouse models and preclinical studies, XL184 demonstrates robust antiangiogenic, antitumor, and anti-invasive effects, dramatically alters tumor pathology, prevents the development of metastases, and reduces tumor burden [1-3].


Technical information:

Chemical Formula:   C28H24FN3O5
CAS #:   849217-68-1
Molecular Weight:   501.51
Purity: > 98%
Appearance:   White
Chemical Name:   N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Solubility:   Up to 22 mM in DMSO
Synonyms:   XL184, XL-184, BMS-907351, BMS907351, Cabozantinib, Cometriq

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor,simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011. 10(12):2298-308. Pubmed ID: 21926191
2. Herreros-Villanueva M, et al. c-Met in pancreatic cancer stem cells: Therapeutic implications. World J Gastroenterol. 2012. 18(38):5321-3. Pubmed ID: 23082047
3. Kurzrock R,et al. Activity of XL184 (Cabozantinib), an oral tyrosine kinase inhibitor, in patients with medullary thyroid cancer. J Clin Oncol. 2011. 29(19):2660-6. Pubmed ID: 21606412

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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