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西特拉瓦替尼（MGCD516）

VEGFR3 选择性抑制剂
规格或纯度: 96%
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货号 (SKU) 包装规格 是否现货 价格 数量
S414066-5mg
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S414066-10mg
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S414066-25mg
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S414066-50mg
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S414066-100mg
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AXL receptor tyrosine kinase Inhibitor discoidin domain receptor tyrosine kinase 2 Inhibitor EPH receptor A3 Inhibitor fms related receptor tyrosine kinase 1 Inhibitor fms related receptor tyrosine kinase 3 Inhibitor fms related receptor tyrosine kinase 4 Inhibitor kinase insert domain receptor Inhibitor KIT proto-oncogene，receptor tyrosine kinase Inhibitor MER proto-oncogene，tyrosine kinase Inhibitor MET proto-oncogene，receptor tyrosine kinase Inhibitor neurotrophic receptor tyrosine kinase 1 Inhibitor platelet derived growth factor receptor alpha Inhibitor
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基本描述

规格或纯度 96%
英文名称 Sitravatinib (MGCD516)
别名 MG516；N-(3-Fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
英文别名 MG516；N-(3-Fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
生化机理 Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Information

Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multipleRTKsinvolved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.


Targets

DDR2 (Cell-free assay); EPHA3 (Cell-free assay); Axl (Cell-free assay); Mer (Cell-free assay); VEGFR3 (FLT4) (Cell-free assay) 27977,0.5 nM; 1 nM; 1.5 nM; 2 nM; 2 nM


In vitro

MGCD516 (Sitravatinib), is an oral, potent small molecule inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (VEGFR, PDGFR and KIT), TRK family, DDR2, MET and AXL. MGCD516 treatment resulted in significant blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.


In vivo

Sitravatinib has demonstrated antitumor activity in nonclinical cancer models harboring genetic alterations of sitravatinib targets, including rearrangement of RET, NTRK, or CHR4q12 amplification. MGCD516 treatment of tumor xenografts in vivo resulted in significant suppression of tumor growth. Efficacy of MGCD516 was superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.


Cell Research(from reference)

Cell lines：DDLS, LS141 and MPNST?

Concentrations：62.5, 125, 250, 500, 1000, 2000 nM/L?

Incubation Time：72 h?

名称和标识符

IUPAC Name 1-N'-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
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)
InChi Key WLAVZAAODLTUSW-UHFFFAOYSA-N
Canonical SMILES COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
PubChem CID 25212148
分子量 629.68

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 100 mg/mL (158.81 mM); Ethanol: 100 mg/mL (158.81 mM); Water: Insoluble;

关联配体

Ligand ID 9920
名称 sitravatinib
别名 GCD516
类别 Synthetic organic
学名 1-N'-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
生物活性评价 Sitravatinib is reported to produce superior antiproliferative efficacy than and in vitro and in vivo .
A selection of the inhibitory IC50s reported in (Table 1) are included in our table below. In some cases we have restricted our selection to the most potently inhibited isoform from each subfamily of RTKs that were tested.
评价 Sitravatinib (MGCD516) is an inhibitor of multiple receptor tyrosine kinases (RTKs) that was developed as an antineoplatic agent . It targets several RTKs (e.g. c-Met, PDGFR, c-Kit and IGF1-R) whose overexpression has been shown to drive sarcoma cell growth

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参考文献

1. Patwardhan PP, Ivy KS, Musi E, de Stanchina E, Schwartz GK.  (2016)  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,  7  (4):  (4093-109).  [PMID:26675259]
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