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| | Sitravatinib Basic information |
| Product Name: | Sitravatinib | | Synonyms: | Sitravatinib;N-(3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;MGCD-516;MG516;Sitravatinib (MGCD516);CS-2638;1,1-Cyclopropanedicarboxamide, N-[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]-N'-(4-fluorophenyl)-;RTK,MG-516,PD-1,SCFR,DDR1,inhibit,VEGFR2,MG 516,MGCD 516,MER,immune,TRKA,Cluster of differentiation antigen 135,Cancer,Discoidin Domain Receptor,VEGFR3,Inhibitor,Vascular endothelial growth factor receptor,Trk Receptor,Tropomyosin related kinase receptor,CD135,VEGFR,immunotherapy,Macrophages,c-Kit,DDR2,VEGFR1,Tyrosine,Fms like tyrosine kinase 3,FLT3,Axl,TRKB,Sitravatinib,MGCD-516,KIT,kinase,CD117 | | CAS: | 1123837-84-2 | | MF: | C33H29F2N5O4S | | MW: | 629.68 | | EINECS: | | | Product Categories: | | | Mol File: | 1123837-84-2.mol |  |
| | Sitravatinib Chemical Properties |
| Boiling point | 833.5±65.0 °C(Predicted) | | density | 1.417±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to at least 25 mg/ml), or in Ethanol (up to at least 25 mg/ml) | | pka | 13.17±0.70(Predicted) | | form | solid | | color | Off-white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
| | Sitravatinib Usage And Synthesis |
| Description | Sitravatinib is a multi-kinase inhibitor. It inhibits 35 kinases (IC50s = 0.5-5,550 nM) in a panel of 55 receptor tyrosine kinases (RTKs). Sitravatinib reduces proliferation of A-673, LPS141, MPNST, DDLS, and Saos-2 cancer cells (IC50s = 1,750, 340.1, 705.7, 266, and 1,830 nM, respectively) and decreases phosphorylation of insulin-like growth factor 1 receptor (IGF1-R), PDGFRβ, and Akt in these same cells when used at concentrations ranging from 62.5 to 4,000 nM. It decreases tumor growth in LPS141 and MPNST mouse xenograft models when administered at a dose of 15 mg/kg per day. | | Description | Sitravatinib, known as MGCD516, is a multikinase (MET, RET, AXL, NTRK1, or NTRK3 genes) inhibitor used in a phase 1/1b clinical trial (NCT02219711) for patients with advanced cancers (NCT02219711). | | Uses | MGCD 516 is an intermediate used to prepare substituted thienopyridines as inhibitors of protein tyrosine kinase activity. | | References | 1) Parag?et al.?(2016)?Significant blockade of multiple receptor kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma; Oncotarget?7?4093
2) Leal?et al.?(2017)?Evidence of clinical activity of sitravatinib in combination with nivolumab in NSCLC patients progressing on prior checkpoint inhibitors; J. Thorac. Oncol.?12?S1803
3) Du?et al.?(2018);?Sitravatinib potentiates immune checkpoint blockade in refractory cancer models; JCI Insight?3?124184 |
| | Sitravatinib Preparation Products And Raw materials |
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