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Sitravatinib
$60 – $680
Products Details
Product Description
– Sitravatinib (MGCD516) 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 shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].
Web ID
– HY-16961
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C33H29F2N5O4S
References
– [1]Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21). pii: 124184.|[2]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.
CAS Number
– 1123837-84-2
Molecular Weight
– 629.68
Compound Purity
– 99.59
SMILES
– 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
– DMSO : ≥ 32 mg/mL
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.
