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Sitravatinib

Sitravatinib

产品编号 T4349   CAS 1123837-84-2
别名: MG516, MGCD516

Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶抑制剂。它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。

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Sitravatinib Chemical Structure
Sitravatinib, CAS 1123837-84-2
规格 价格/CNY 货期 数量
1 mg ¥ 217 现货
5 mg ¥ 477 现货
10 mg ¥ 745 现货
25 mg ¥ 1,390 现货
50 mg ¥ 2,230 现货
100 mg ¥ 3,570 现货
200 mg ¥ 5,190 现货
500 mg ¥ 7,920 现货
1 mL * 10 mM (in DMSO) ¥ 686 现货
其他形式的 Sitravatinib:
产品目录号及名称: Sitravatinib (T4349)
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纯度: 99.74%
纯度: 99.67%
纯度: 98.9%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Sitravatinib (MGCD516) (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
靶点活性 Axl:1.5 nM, VEGFR3 (FLT4):2 nM, Mer:2 nM, EPHA3:1 nM, DDR2:0.5 nM
体外活性 MGCD516 (Sitravatinib) is an inhibitor of a closely related spectrum of RTKs including RET, the split RTKs (PDGFR, VEGFR, and KIT), DDR2, TRK family, MET, and AXL. MGCD516 causes the marked blockade of phosphorylation of potential driver RTKs and induced potent anti-proliferative effects in vitro.
体内活性 Sitravatinib has antitumor activity in nonClinicalal cancer models harboring genetic alterations of sitravatinib targets, including the rearrangement of NTRK, RET, or CHR4q12 amplification. In vivo tumor xenografts, MGCD516 causes the significant suppression of tumor growth. Efficacy of MGCD516 is superior to imatinib and crizotinib, two other well-studied multi-kinase inhibitors with overlapping target specificities, both in vitro and in vivo.
细胞实验 Cell lines: DDLS,LS141,and MPNST. Concentrations: 62.5,125,250,500,1000,2000 nM2,000-3,000 cells were plated in 96-well plates in RPMI/DME media with 10% FBS and then treated with the indicated drugs the next day.After 72 hours,media was replaced with 100 μL of media with 10% serum and 10% CCK-8 solution.After 1 hour,the optical density was read at 450 nm to determine viability.Background values from negative control wells without cells were subtracted for final sample quantification.Data was plotted as % cell viability compared to DMSO control.
动物实验 Animal Models: ICR/SCID mice. Formulation: 0.5% hydroxypropyl methylcellulose (HPMC) and 0.1% Tween-80 solution (pH 1.4). Dosages: 15 mg/kg. Administration: p.o.
别名 MG516, MGCD516
分子量 629.68
分子式 C33H29F2N5O4S
CAS No. 1123837-84-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 32 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

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 preClinicalal models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.

文献引用

1. Zhang Y, Wang P, Wang Y, et al.Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia.Biomarker Research.2023, 11(1): 1-16.
Brigatinib R406 free base Sunitinib SKLB4771 3-Hydroxy Midostaurin Merestinib SB1317 hydrochloride (1204918-72-8(free base)) R1530

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌药物库 抗乳腺癌化合物库 临床期小分子药物库 含氟化合物库 抗肝癌化合物库 抑制剂库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Sitravatinib 1123837-84-2 Angiogenesis Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) VEGFR FLT Trk receptor TAM Receptor c-Kit Ephrin Receptor RTK PD-1 SCFR DDR1 inhibit VEGFR2 MER immune TRKA Cluster of differentiation antigen 135 Cancer Discoidin Domain Receptor VEGFR3 Inhibitor Vascular endothelial growth factor receptor MG516 Trk Receptor Tropomyosin related kinase receptor CD135 MGCD 516 immunotherapy Macrophages MG-516 MGCD-516 DDR2 MGCD516 VEGFR1 Tyrosine MG 516 Fms like tyrosine kinase 3 FLT3 Axl TRKB KIT kinase CD117 inhibitor

 

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