Sitravatinib
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].
Product Specifications
CAS Number
1123837-84-2
Product Name Alternative
MGCD516; MG-516
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
C-Kit; Discoidin Domain Receptor; FLT3; Trk Receptor; VEGFR
Type
Reference compound
Related Pathways
Neuronal Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/Sitravatinib.html
Purity
99.57
Solubility
DMSO : ≥ 32 mg/mL
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
Molecular Formula
C33H29F2N5O4S
Molecular Weight
629.68
Precautions
H302, H315, H319, H335
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
DDR1; DDR2; TrkA; TrkB; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
Available Sizes
Frequently Asked Questions
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