Sitravatinib
Cat. No.：YN380118
CAS No. ：1123837-84-2
| 产品名称: | Sitravatinib |
| CAS No.: | 1123837-84-2 |
| Chemical Name: | N-[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide |
| Synonyms: | MGCD516; MG-516 |
| 分子量: | 629.68 |
| 分子式: | C₃₃H₂₉F₂N₅O₄S |
| 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 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶 (RTK) 抑制剂。抑制 Axl，MER，VEGFR3，VEGFR2，VEGFR1，KIT，FLT3，DDR2，DDR1，TRKA，和 TRKB，IC50分别为 1.5 nM，2 nM，2 nM，5 nM，6 nM，6 nM，8 nM，0.5 nM，29 nM，5 nM，和 9 nM。Sitravatinib 单独使用即具有有效的抗肿瘤功效，且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。 |
| IC50和靶点: | [{name:"Axl:1.5 nM (IC50)"},{name: "MER:2 nM (IC50)"},{name: "VEGFR3:2 nM (IC50)"},{name: "VEGFR2:5 nM (IC50)"},{name: "VEGFR1:6 nM (IC50)"},{name: "TrkA:5 nM (IC50)"},{name: "TrkB:9 nM (IC50)"},{name: "KIT:6 nM (IC50)"},{name: "FLT3:8 nM (IC50)"},{name: "DDR2:0.5 nM (IC50)"},{name: "DDR1:29 nM (IC50)"}] |
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Patwardhan, P.P., Ivy, K.S., Musi, E., 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 sarcomaOncotarget7(4),4093-4109(2016)
