Tyrosine Kinase/Adaptors Tyrosine Kinases Sitravatinib


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

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

Sitravatinib, CAS 1123837-84-2
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 80.00
10 mg In stock 120.00
25 mg In stock 248.00
50 mg In stock 300.00
100 mg Inquiry 490.00
200 mg Inquiry 820.00
1 mL * 10 mM (in DMSO) In stock 110.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sitravatinib (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 DDR2,   EPHA3,   Axl,   Mer,   VEGFR3 (FLT4),  
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.
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.
Animal Model:
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.
Cell lines:
Synonyms MG516 , MGCD516 , MGCD516 MG516
Purity 99.67%
Molecular Weight 629.68
Formula C33H29F2N5O4S
CAS No. 1123837-84-2


0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )


References 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. 2. Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21). pii: 124184.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Anti-cancer Compound Library Clinical Compound Library Anti-cancer Clinical Compound Library

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