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PHA-665752

PHA-665752

产品编号 T6128   CAS 477575-56-7
别名: PHA 665752, PHA665752

PHA-665752 是一种选择性的 ATP 竞争活性位点 c-Met 激酶抑制剂,Ki 为 4 nM,IC50为 9 nM。它对 c-Met 的选择性比一组不同的酪氨酸和丝氨酸苏氨酸激酶高 50 倍。它诱导细胞凋亡细胞周期阻滞,具有细胞还原性抗肿瘤活性。

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PHA-665752 Chemical Structure
PHA-665752, CAS 477575-56-7
规格 价格/CNY 货期 数量
1 mg ¥ 208 现货
5 mg ¥ 478 现货
10 mg ¥ 762 现货
25 mg ¥ 1,580 现货
50 mg ¥ 2,980 现货
100 mg ¥ 4,590 现货
1 mL * 10 mM (in DMSO) ¥ 785 现货
产品目录号及名称: PHA-665752 (T6128)
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纯度: 99.35%
纯度: 97.05%
纯度: 97.01%
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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 PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
靶点活性 c-Met:9 nM
体外活性 PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. PHA-665752 potently inhibits the HGF-stimulated c-Met autophosphorylation with IC50 of 25-50 nM. PHA-665752 also significantly blocks HGF- and c-Met-dependent functions such as cell motility and cell proliferation with IC50 of 40-50 nM and 18-42 nM, respectively. In addition, PHA-665752 potently inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines. [1] PHA-665752 inhibits cell growth in TPR-MET-transformed BaF3 cells with IC50 of <60 nM, and inhibits constitutive cell motility and migration by 92.5% at 0.2 μM. Inhibition of c-Met by PHA665752 (0.2 μM) also induces cell apoptosis of 33.1% and G1 cell cycle arrest with cells in G1 phase increasing from 42.4% to 77.0%. PHA665752 can cooperate with rapamycin to inhibit cell growth of TPR-MET-transformed BaF3 cells and non-small cell lung cancer H441 cells. [2]
体内活性 Administration of PHA-665752 induces a dose-dependent tumor growth inhibition of S114 xenografts by 20 %, 39% and 68%, at dose of 7.5, 15, and 30 mg/kg/day, respectively. [1] PHA665752 treatment significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively. PHA665752 also significantly inhibits angiogenesis by >85%, due to decreasing the production of vascular endothelial growth factor and increasing the production of the angiogenesis inhibitor thrombospondin-1. [3]
激酶实验 In vitro enzyme assay: The c-Met kinase domain GST-fusion protein is used for the c-Met assay. The IC50 value of PHA-665752 for the inhibition of c-Met is based on phosphorylation of kinase peptide substrates or poly-glu-tyr in the presence of ATP and divalent cation (MgCl2 or MnCl2 10-20 mM). The linear range (i.e., the time period over which the rate remains equivalent to the initial rate) is determined for c-Met, and the kinetic measurement and IC50 determination are performed within this range.
细胞实验 For proliferation assays, cells are grown in medium with 0.1% FBS for 48 hours after which they are treated with various concentrations of PHA-665752 in HGF (50 ng/mL) in a medium containing 2% FBS. After 18 hours, cells are incubated with BrdUrd for 1 hour, fixed, and stained with anti-BrdUrd peroxidase-conjugated antibody, and plates are read at 630 nm. For apoptosis assays, cells are grown in medium with 2% FBS in presence and absence of HGF (50 ng/mL) and various concentrations of PHA-665752 for 72 hours. After 72 hours, a mixture containing ethidium bromide and acridine orange is added, and apoptotic cells (bright orange cells or cell fragments) are counted by fluorescence microscopy.(Only for Reference)
别名 PHA 665752, PHA665752
分子量 641.61
分子式 C32H34Cl2N4O4S
CAS No. 477575-56-7

存储

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

溶解度

DMSO: 64.2 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5586 mL 7.7929 mL 15.5858 mL 38.9645 mL
5 mM 0.3117 mL 1.5586 mL 3.1172 mL 7.7929 mL
10 mM 0.1559 mL 0.7793 mL 1.5586 mL 3.8964 mL
20 mM 0.0779 mL 0.3896 mL 0.7793 mL 1.9482 mL
50 mM 0.0312 mL 0.1559 mL 0.3117 mL 0.7793 mL
100 mM 0.0156 mL 0.0779 mL 0.1559 mL 0.3896 mL

计算器

摩尔浓度计算器
稀释计算器
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分子量计算器
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参考文献

1. Christensen JG, et al. Cancer Res, 2003, 63(21), 7345-7355. 2. Ma PC, et al. Clin Cancer Res, 2005, 11(6), 2312-2319. 3. Puri N, et al. Cancer Res, 2007, 67(8), 3529-3534.

文献引用

1. Yuan S, Gong Y, Chen R, et al. Chinese herbal formula QHF inhibits hepatocellular carcinoma metastasis via HGF/c-Met signaling pathway. Biomedicine & Pharmacotherapy. 2020, 132: 110867.
L-Ascorbic acid 2-phosphate trisodium SGI-7079 BMS-754807 AMG-458 Davutamig 1D228 PF-04217903 phenolsulfonate SAR125844

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 酪氨酸激酶分子库 经典已知活性库 抗癌化合物库 成骨分子库 激酶抑制剂库 临床前化合物库 细胞因子抑制剂库 NO PAINS 化合物库 抗结直肠癌化合物库

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
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% Tween 80
% ddH2O
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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

PHA-665752 477575-56-7 Angiogenesis Apoptosis Autophagy Cytoskeletal Signaling Tyrosine Kinase/Adaptors VEGFR FGFR c-Met/HGFR Bcr-Abl Inhibitor inhibit PHA 665752 PHA665752 inhibitor

 

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