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Sitravatinib

Sitravatinib

Item no.	HY-16961-25mg
Manufacturer	MedChem Express
CASRN	1123837-84-2
Amount	25 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 200 mg 25 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.57
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.
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	MGCD516,MG-516
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	c-Kit; Discoidin Domain Receptor; FLT3; Trk Receptor; VEGFR
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	629.68
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].
Manufacturer - Research Area	Cancer; Inflammation/Immunology
Solubility	DMSO: ≥ 32 mg/mL
Manufacturer - Pathway	Neuronal Signaling; Protein Tyrosine Kinase/RTK
Isoform	DDR1; DDR2; TrkA; TrkB; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
Clinical information	Phase 3

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HY-16961-25mg-safety-datasheet.pdf