SGX-523 | MET Inhibitor | AmBeed-信号通路专用抑制剂

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SGX-523 {[allProObj[0].p_purity_real_show]}

货号：A263510

SGX-523 is a potent and selective c-Met inhibitor with IC50 of 4 nM.

SGX-523 化学结构
CAS号：1022150-57-7

SGX-523 3D分子结构
CAS号：1022150-57-7

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SGX-523 纯度/质量文件产品仅供科研

货号：A263510 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

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SGX-523 生物活性

描述

Hepatocyte growth factor (HGF) receptor, c-Met, is the prototypic member of a family of receptor tyrosine kinases unique to deuterostomes and has emerged as an important target for the development of novel cancer therapeutics. SGX523 is a novel, ATP-competitive and selective c-Met inhibitor with an IC₅₀ of 4 nM and a K_i of 2.7 nM. In the gastric cancer cell line GTL16, c-Met gene amplification led to constitutive signaling, which was abolished by SGX523 with an IC₅₀ of 0.04 μM. SGX523 also abrogated HGF induced signaling in A549 lung cancer cells with an IC₅₀ of 0.012 μM for the inhibition of c-Met autophosphorylation. Further, SGX523 inhibited the growth of gastric and lung cancer cell lines with amplification of the c-Met gene. In vivo, SGX523 significantly retarded the growth of preestablished GTL16 tumors when administered orally at doses of ≥10 mg/kg twice daily. Moreover, SGX523 (10 mg/kg; twice daily) potently inhibited U87MG tumor growth; SGX523 (30 mg/kg; twice daily) led to clear regression of U87MG tumors^[3].

作用机制

SGX-523 binds to the ATP site of an inactive conformation^[3].

SGX-523 参考文献

[1]Shen A, Wang L, et al. c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. Cancer Res. 2015 Nov 1;75(21):4548-59.

[2]Buchanan SG, Hendle J, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther. 2009 Dec;8(12):3181-90.

[3]Buchanan SG, Hendle J, Lee PS, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther. 2009 Dec;8(12):3181-90

SGX-523 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.91mL

2.78mL

1.39mL

27.82mL

5.56mL

2.78mL

SGX-523 技术信息

CAS号	1022150-57-7
分子式	C₁₈H₁₃N₇S
分子量	359.41
SMILES Code	CN1N=CC(C2=NN3C(C=C2)=NN=C3SC4=CC=C5N=CC=CC5=C4)=C1
MDL No.	MFCD16660190

别名
运输	蓝冰
InChI Key	BCZUAADEACICHN-UHFFFAOYSA-N
Pubchem ID	24779724

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

动物实验配方

0.5% methylcellulose+0.2% Tween 80+water 30 mg/mL suspension

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浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

浓度

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分子量

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SGX-523 {[allProObj[0].p_purity_real_show]}

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SGX-523 {[allProObj[0].p_purity_real_show]}

SGX-523 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SGX-523 质控信息

SGX-523 生物活性

SGX-523 参考文献

SGX-523 实验方案

SGX-523 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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