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Sitravatinib malate

Catalog No. T12925 CAS 2244864-88-6

Synonyms: MGCD516 malate, MG-516 malate

Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

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Sitravatinib malate, CAS 2244864-88-6

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
Targets&IC50	TrkA:5 nM, FLT3:8 nM, TrkB:9 nM, DDR2:0.5 nM, c-Kit:6 nM, DDR1:29 nM, VEGFR1:6 nM, Mer:2 nM, Axl:1.5 nM, VEGFR3:2 nM, VEGFR2:5 nM
In vitro	In KLN205 and E0771 cell lines,Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner [2]. Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability(IC50s : 1 μM, in KLN205), E0771 and CT1B-A5 cell lines[2].
In vivo	In C57BL/6 mice bearing CT1B-A5 cells model,Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression [2].

Synonyms	MGCD516 malate, MG-516 malate
Molecular Weight	763.76
Formula	C37H35F2N5O9S
CAS No.	2244864-88-6

Storage

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

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 preclinical 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.

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Keywords

Sitravatinib malate 2244864-88-6 Tyrosine Kinase/Adaptors TAM Receptor MG-516 Malate MGCD-516 Malate MGCD516 Malate MG516 Malate MGCD 516 Malate MG 516 Malate MGCD516 malate Sitravatinib Malate MG-516 malate inhibitor inhibit

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