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Cabozantinib (BMS-907351) - 10mM in DMSO, high purity , CAS No.849217-68-1(DMSO), Inhibitor of kinase insert domain receptor;Inhibitor of MET proto-oncogene; receptor tyrosine kinase;Inhibitor of ret proto-oncogene

COA COA
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Item Number
C408733
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C408733-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$289.90
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VEGFR2 Selective Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms XL184 | N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabo
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of kinase insert domain receptor;Inhibitor of MET proto-oncogene; receptor tyrosine kinase;Inhibitor of ret proto-oncogene
Product Description

Information

Cabozantinib (XL184, BMS-907351) is a potentVEGFR2inhibitor withIC50of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL withIC50of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantin
In vitro

XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. XL184 at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. XL184 also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although XL-184 has no significant effect on MPNST cell growth at 0.1 μM, XL184 at 5-10 μM significantly inhibits the MPNST cell growth.

In vivo

XL184 treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. XL184 also decreases invasiveness of primary tumors and reduces metastasis. XL184 at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. Administration of XL184 induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of XL184 is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively.
Cell Data

cell lines：A549 and H1299 cell

Concentrations：Dissolved in DMSO, final concentrations ~10 μM

Incubation Time：48 hours

Powder Purity:≥99%

Product Properties

ALogP 4.342
hba_count 6
HBD Count 2
Rotatable Bond 8

Associated Targets(Human)

EGFR Tclin Epidermal growth factor receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (15 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT4 Tclin Vascular endothelial growth factor receptor 3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FGFR1 Tclin Fibroblast growth factor receptor 1 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MET Tclin Hepatocyte growth factor receptor (20 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
TEK Tclin Angiopoietin-1 receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
BCR Tclin Breakpoint cluster region protein (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (20 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (6 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KIT Tclin Mast/stem cell growth factor receptor Kit (6 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles COC1=CC2=C(C=C1OC)C(=CC=N2)OC3=CC=C(NC(=O)C4(CC4)C(=O)NC5=CC=C(F)C=C5)C=C3
Molecular Weight 501.51
Reaxy-Rn 18631644
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18631644&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro      
DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 199.4
Water(mg / mL) Max Solubility <1

Solution Calculators

Reviews

Customer Reviews

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