Catalog No.S8573 Synonyms: MG-516
Molecular Weight(MW): 629.68
Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
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|Description||Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.|
MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.
|In vivo||Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.|
|In vitro||DMSO||100 mg/mL (158.81 mM)|
|Ethanol||100 mg/mL (158.81 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03606174||Recruiting||Urothelial Carcinoma|Urothelial Carcinoma Bladder|Urothelial Carcinoma Ureter|Urothelial Carcinoma of the Renal Pelvis and Ureter|Urothelial Carcinoma Urethra||Mirati Therapeutics Inc.||August 9 2018||Phase 2|
|NCT03575598||Recruiting||Squamous Cell Carcinoma Head And Neck|Squamous Cell Carcinoma Mouth|Squamous Cell Carcinoma of the Oral Cavity||University Health Network Toronto|Mirati Therapeutics Inc.||August 30 2018||Early Phase 1|
|NCT03015740||Recruiting||Malignant Neoplasms of Urinary Tract|Other Disorders of Kidney and Ureter|Renal Cell Carcinoma||M.D. Anderson Cancer Center|Mirati Therapeutics Inc.|Gateway for Cancer Research||April 23 2017||Phase 1|Phase 2|
|NCT02978859||Recruiting||Liposarcoma|Metastatic Liposarcoma||Gary Schwartz|Mirati Therapeutics Inc.|Columbia University||November 2016||Phase 2|
|NCT02954991||Recruiting||Carcinoma Non-Small-Cell Lung||Mirati Therapeutics Inc.||November 2016||Phase 2|
|NCT02219711||Recruiting||Advanced Cancer||Mirati Therapeutics Inc.||August 2014||Phase 1|
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