Sitravatinib
- Product Name
- Sitravatinib
- CAS No.
- 1123837-84-2
- Chemical Name
- Sitravatinib
- Synonyms
- MG516;CS-2638;MGCD-516;Sitravatinib;MGCD516 (SITRAVATINIB);Sitravatinib (MGCD516);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;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
- CBNumber
- CB03128970
- Molecular Formula
- C33H29F2N5O4S
- Formula Weight
- 629.68
- MOL File
- 1123837-84-2.mol
Sitravatinib Property
- 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)
- form
- solid
- pka
- 13.17±0.70(Predicted)
- 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.
N-Bromosuccinimide Price
- Product number
- 27338
- Product name
- Sitravatinib
- Packaging
- 5mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 27338
- Product name
- Sitravatinib
- Packaging
- 10mg
- Price
- $107
- Updated
- 2024/03/01
- Product number
- 27338
- Product name
- Sitravatinib
- Packaging
- 25mg
- Price
- $233
- Updated
- 2024/03/01
- Product number
- 27338
- Product name
- Sitravatinib
- Packaging
- 50mg
- Price
- $437
- Updated
- 2024/03/01
- Product number
- 456189
- Product name
- MGCD 516
- Packaging
- 10mg
- Price
- $425
- Updated
- 2021/12/16
Sitravatinib Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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