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Cabozantinib malate (XL184) - 10mM in DMSO, high purity , CAS No.1140909-48-3(DMSO), Hepatocyte growth factor receptor inhibitor

COA

Grade & Purity:

10mM in DMSO

Cas Number: 1140909-48-3(DMSO)
Molecular Weight: 635.59

In stock

Item Number

C408163

Grouped product items
SKU	Size	Availability	Price	Qty
C408163-1ml	1ml	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$261.90

VEGFR2 Selective Inhibitors

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Compound libraries (12325)

Basic Description

Synonyms	Butanedioic acid, 2-hydroxy-, (2S)-, compd. with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1)
Specifications & Purity	10mM in DMSO
Biochemical and Physiological Mechanisms	Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-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
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.
Action Type	INHIBITOR
Mechanism of action	Hepatocyte growth factor receptor inhibitor
Product Description	Information Cabozantinib malate (XL184) is the malate of Cabozantinib, a potentVEGFR2inhibitor withIC50of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-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 cel In vitro Cabozantinib 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. Cabozantinib 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. Cabozantinib also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although Cabozantinib has no significant effect on MPNST cell growth at 0.1 μM, Cabozantinib at 5-10 μM significantly inhibits the MPNST cell growth. In vivo Cabozantinib 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. Cabozantinib also decreases invasiveness of primary tumors and reduces metastasis. Cabozantinib at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. Administration of Cabozantinib 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 Cabozantinib 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： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：48 hours Powder Purity:≥99%

Product Properties

ALogP	3.331
hba_count	8
HBD Count	3
Rotatable Bond	11

Associated Targets(Human)

MET Tclin Hepatocyte growth factor receptor (2 Activities)

Discover Target: MET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)

Discover Target: KDR

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.OC(CC(O)=O)C(O)=O
Molecular Weight	635.59
Reaxy-Rn	20538690
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20538690&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: 30 mg/mL (92.09 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	100
DMSO(mM) Max Solubility	157.33
Water(mg / mL) Max Solubility	<1

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