Cabozantinib malate (XL184)
For research use only.
CAS No. 1140909-48-3
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 in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.
Selleck's Cabozantinib malate (XL184) has been cited by 66 publications
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|Description||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 in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.|
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. |
|In vitro||DMSO||100 mg/mL (157.33 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04868773||Not yet recruiting||Drug: Cabozantinib|Drug: TAS-102||Colorectal Cancer|Colorectal Carcinoma|Metastatic Cancer|CRC||University of California Irvine||July 2021||Phase 1|
|NCT04804813||Recruiting||Drug: Cabozantinib||Renal Cell Carcinoma||Takeda||March 29 2021||--|
|NCT04631744||Recruiting||Drug: Cabozantinib||Prostate Cancer||Weill Medical College of Cornell University|Exelixis||March 3 2021||Phase 2|
|NCT04551430||Recruiting||Drug: Cabozantinib|Drug: Nivolumab|Drug: Ipilimumab||Metastatic Soft-tissue Sarcoma||Washington University School of Medicine|Exelixis|Bristol-Myers Squibb||January 5 2021||Phase 2|
|NCT04524208||Not yet recruiting||Drug: Cabozantinib||Neuroendocrine Tumors|Neuroendocrine Carcinoma||Karsten Gavenis|University Medical Center Goettingen||December 1 2020||Phase 2|
|NCT04637204||Completed||Drug: Cabozantinib|Drug: Axitinib||Renal Cell Carcinoma||Ipsen||November 24 2020||--|
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