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Products Details
Product 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].
Web ID
– HY-16961A
Shipping
– Room temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C37H35F2N5O9S
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.
CAS Number
– 2244864-88-6
Molecular Weight
– 763.76
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
Clinical Information
– Phase 3
Research Area
– Cancer; Inflammation/Immunology
Solubility
– 10 mM in DMSO
Target
– c-Kit;Discoidin Domain Receptor;FLT3;Trk Receptor;VEGFR
Isoform
– DDR1;DDR2;TrkA;TrkB;VEGFR1/Flt-1;VEGFR2/KDR/Flk-1;VEGFR3/Flt-4
Pathway
– Neuronal Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
