MGCD516
- Sitravatinib
- Soluble in DMSO
- MF: C33H29F2N5O4S
- MW: 629.68
Description
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. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
More Information
| Parent CAS No. | 1123837-84-2 |
|---|---|
| Chemical Name | N-(3-fluoro-4-(2-(5-((2-methoxyethylamino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1N=C2C=C(C3N=CC(CNCCOC)=CC=3)SC2=C(OC2C=CC(NC(=O)C3(CC3)C(=O)NC3C=CC(F)=CC=3)=CC=2F)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42) |
| InChiKey | WLAVZAAODLTUSW-UHFFFAOYSA-N |
| CID | 25212148 |
| Short Description | RTK inhibitor |
References
- PP Patwardhan 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.
- W Du et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21):e124184.
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