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BMS-777607

现货
Catalog No.
A5703
强效的c-Met选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 850.00
Ship with 10-15 days
5mg
¥ 800.00
Ship with 10-15 days
25mg
¥ 2,500.00
Ship with 10-15 days
100mg
¥ 6,800.00
Ship with 10-15 days

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Background

BMS 777607 is a novel, selective and orally available ATP-competitive MET kinase inhibitor that primarily targets several MET family members, including RON, MET, Tyro-3 and AxI, with half maximal inhibitory concentration IC50 of 1.8 nmol/L, 3.9 nmol/L, 4.3 nmol/L and 1.1 nmol/L respectively. Moreover, at higher concentrations, BMS 777607 has been found to inhibit other protein tyrosine kinases, including Mer, Flt-3, Aurora B, Lck and VEGFR2 with IC50 of 14 nmol/L, 16 nmol/L, 78 nmol/L, 120 nmol/L and 180 nmol/L respectively. In previous studies, BMS 777607 potently inhibited the auto-phosphorylation of c-MET (IC50: 20 nmol/L) leading to impaired xenograft growth.

References:
[1]Dai Y, Siemann DW. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther. 2010 Jun;9(6):1554-61. doi: 10.1158/1535-7163.MCT-10-0359. Epub 2010 Jun 1.
[2]Sharma S, Zeng JY, Zhuang CM, Zhou YQ, Yao HP, Hu X, Zhang R, Wang MH.

Small-molecule inhibitor BMS-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents. Mol Cancer Ther. 2013 May;12(5):725-36. doi: 10.1158/1535-7163.MCT-12-1079. Epub 2013 Mar 6.

文献引用

1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt512.89
Cas No.1025720-94-8
FormulaC25H19ClF2N4O4
Solubility≥25.65mg/mL in DMSO, <2.78 mg/mL in EtOH, <2.4 mg/mL in H2O
Chemical NameN-[4-(2-amino-3-chloropyridin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide
SDFDownload SDF
Canonical SMILESCCOC1=C(C(=O)N(C=C1)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

KHT细胞

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

10 μM;2、24和96小时

实验结果

在具有高度转移性的鼠科KHT细胞中,给予~ 10 μM BMS-777607,于2小时后,显著降低自磷酸化c-Met水平,

动物实验 [1]:

动物模型

KHT细胞异种移植小鼠模型

给药剂量

10 ~ 25 mg/kg;口服给药;每日1次

实验结果

在KHT细胞异种移植小鼠模型中,BMS-777607 (25 mg/kg/day) 降低KHT肺肿瘤结节数量 (28.3%),改善形态性出血,同时,显著破坏转移表型。此外,BMS-777607无明显毒性。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Dai Y, Bae K, Pampo C, Siemann DW. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Clin Exp Metastasis. 2012 Mar;29(3):253-61.

生物活性

描述 BMS-777607是Met相关激酶的抑制剂,作用于c-Met、Axl、Ron和Tyro3 ,对应的IC50值为3.9 nM、1.1 nM、1.8 nM和4.3 nM。对Met相关靶点的选择性比对Lck、VEGFR-2和TrkA/B高40倍,比对其它受体和非受体激酶的选择性高500多倍。
靶点 c-Met Axl Ron Tyro3    
IC50 3.9 nM 1.1 nM 1.8 nM 4.3 nM    

质量控制

质量控制和MSDS

批次:

化学结构

BMS-777607

相关生物数据

BMS-777607

相关生物数据

BMS-777607