Sitravatinib malate

Modify Date: 2024-01-10 14:50:01

Sitravatinib malate Structure
Sitravatinib malate structure
Common Name Sitravatinib malate
CAS Number 2244864-88-6 Molecular Weight 763.76
Density N/A Boiling Point N/A
Molecular Formula C37H35F2N5O9S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Sitravatinib malate


Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with 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[1]. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].

 Names

Name Sitravatinib malate

 Sitravatinib malate Biological Activity

Description Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with 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[1]. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].
Related Catalog
Target

Axl:1.5 nM (IC50)

MER:2 nM (IC50)

VEGFR3:2 nM (IC50)

VEGFR2:5 nM (IC50)

VEGFR1:6 nM (IC50)

TrkA:5 nM (IC50)

TrkB:9 nM (IC50)

KIT:6 nM (IC50)

FLT3:8 nM (IC50)

DDR2:0.5 nM (IC50)

DDR1:29 nM (IC50)

In Vitro Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines[2]. Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines[2]. Cell Viability Assay[2] Cell Line: KLN205, E0771, CT1B-A5 cells Concentration: 0.001, 0.01, 0.1, 1, 10 μM Incubation Time: 5 days Result: Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM.
In Vivo Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model[2]. Animal Model: 6-week-old C57BL/6 mice (bearing CT1B-A5 cells)[2] Dosage: 20 mg/kg Administration: Oral administration; once per day for 6 days Result: Significantly inhibited tumor progression and induced tumor regression.
References

[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.

 Chemical & Physical Properties

Molecular Formula C37H35F2N5O9S
Molecular Weight 763.76
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