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Sitravatinib (malate)

CAT: 0804-HY-16961ASize: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-16961ASize:1 Each
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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].
CAS Number
2244864-88-6
Product Name Alternative
MGCD516 (malate) ; MG-516 (malate)
UNSPSC
12352005
Target
C-Kit; Discoidin Domain Receptor; FLT3; Trk Receptor; VEGFR
Type
Reference compound
Related Pathways
Neuronal Signaling; Protein Tyrosine Kinase/RTK
Applications
COVID-19-immunoregulation
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/sitravatinib-malate.html
Solubility
10 mM in DMSO
Smiles
O=C(O)[C@@H](O)CC(O)=O.O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC=C(OC4=C5C(C=C(C6=NC=C(CNCCOC)C=C6)S5)=NC=C4)C(F)=C3
Molecular Formula
C37H35F2N5O9S
Molecular Weight
763.76
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
DDR1; DDR2; TrkA; TrkB; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

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CatalogName
T12925-01Sitravatinib malate
BS166446-01Sitravatinib
A16259-5Sitravatinib 5mg
S8573-5mgSitravatinib (MGCD516)
A16259-10Sitravatinib 10mg
A16259-50Sitravatinib 50mg

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