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Sitravatinib

Catalog No. T4349   CAS 1123837-84-2
Synonyms: MG516, MGCD516

Sitravatinib (MGCD516) (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

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Sitravatinib Chemical Structure
Sitravatinib, CAS 1123837-84-2
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 72.00
25 mg In stock $ 139.00
50 mg In stock $ 222.00
100 mg In stock $ 355.00
200 mg In stock $ 563.00
500 mg In stock $ 889.00
1 mL * 10 mM (in DMSO) In stock $ 66.00
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Purity: 99.74%
Purity: 99.67%
Purity: 98.9%
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Biological Description
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Storage & Solubility Information
Description Sitravatinib (MGCD516) (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
Targets&IC50 Axl:1.5 nM, VEGFR3 (FLT4):2 nM, Mer:2 nM, EPHA3:1 nM, DDR2:0.5 nM
In vitro MGCD516 (Sitravatinib) is an inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (PDGFR, VEGFR, and KIT), DDR2, TRK family, MET, and AXL. MGCD516 causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.
In vivo Sitravatinib has antitumor activity in nonClinicalal cancer models harboring genetic alterations of sitravatinib targets, including the rearrangement of NTRK, RET, or CHR4q12 amplification. In vivo tumor xenografts, MGCD516 causes the significant suppression of tumor growth. Efficacy of MGCD516 is superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.
Cell Research Cell lines: DDLS,LS141,and MPNST. Concentrations: 62.5,125,250,500,1000,2000 nM2,000-3,000 cells were plated in 96-well plates in RPMI/DME media with 10% FBS and then treated with the indicated drugs the next day.After 72 hours,media was replaced with 100 μL of media with 10% serum and 10% CCK-8 solution.After 1 hour,the optical density was read at 450 nm to determine viability.Background values from negative control wells without cells were subtracted for final sample quantification.Data was plotted as % cell viability compared to DMSO control.
Animal Research Animal Models: ICR/SCID mice. Formulation: 0.5% hydroxypropyl methylcellulose (HPMC) and 0.1% Tween-80 solution (pH 1.4). Dosages: 15 mg/kg. Administration: p.o.
Synonyms MG516, MGCD516
Molecular Weight 629.68
Formula C33H29F2N5O4S
CAS No. 1123837-84-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32 mg/mL

TargetMolReferences and Literature

1. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preClinicalal models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.

TargetMolCitations

1. Zhang Y, Wang P, Wang Y, et al.Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia.Biomarker Research.2023, 11(1): 1-16.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Breast Cancer Compound Library Clinical Compound Library Fluorochemical Library Anti-Liver Cancer Compound Library Inhibitor Library NO PAINS Compound Library

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Keywords

Sitravatinib 1123837-84-2 Angiogenesis Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) VEGFR TAM Receptor Trk receptor FLT c-Kit Ephrin Receptor RTK PD-1 SCFR DDR1 inhibit VEGFR2 MER immune TRKA Cluster of differentiation antigen 135 Cancer Discoidin Domain Receptor VEGFR3 Inhibitor Vascular endothelial growth factor receptor MG516 Trk Receptor Tropomyosin related kinase receptor CD135 MGCD 516 immunotherapy Macrophages MG-516 MGCD-516 DDR2 MGCD516 VEGFR1 Tyrosine MG 516 Fms like tyrosine kinase 3 FLT3 Axl TRKB KIT kinase CD117 inhibitor

 

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