化合物 BMS-777607|T2699|TargetMol

BMS 777607
1025720-94-8

￥277 1mg 起订

￥393 2mg 起订

￥686 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐

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邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 BMS-777607

英文名称：: BMS 777607

CAS号：: 1025720-94-8

品牌：: TargetMol

产地：: 美国

保存条件：: keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.89%

产品类别：: 抑制剂

货号：: T2699

Product Introduction

Bioactivity

名称	BMS 777607
描述	BMS 777607 (BMS 817378) is a Met-related inhibitor targeting c-Met, Axl, Ron, and Tyro3 with IC50 values of 3.9 nM, 1.1 nM, 1.8 nM, and 4.3 nM, respectively. BMS-777607 has been investigated in basic science research for malignant solid tumors.
细胞实验	KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 ml pipette tip followed by treated with BMS-777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μm pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37 °C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5 × 103/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted. (Only for Reference)
激酶实验	Met Kinase Assay: The kinase reaction consists of baculovirus expressed GST-Met, 3 μg of poly(Glu/Tyr), 0.12 μCi 33P γ-ATP, 1 μM ATP in 30 μL of kinase buffer (20 mM Tris-Cl, 5 mM MnCl2, 0.1 mg/mL BSA, 0.5 mM DTT). Reactions are incubated for 1 hour at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration of 8%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester, and the filters are quantitated using a TopCount 96-well liquid scintillation counter. Dose response curves are generated to determine the concentration required to inhibit 50% of substrate phosphorylation (IC50). BMS 777607 is dissolved at 10 mM in dimethylsulfoxide (DMSO) and evaluated at 10 concentrations, in duplicate.
体外活性	在携带GTL-16人类移植瘤的无胸腺小鼠中,BMS-777607（6.25-50 mg/kg,p.o.）可无毒性地显著降低肿瘤体积.BMS 777607（10 mg/kg）也可一定程度抑制肺结节形成.在6-8周大的注射啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠体内,BMS-777607（25 mg/kg/day）降低KHT肺肿瘤结节数量,提高形态出血,且明显修复损害转移表型,且无明显毒性.
体内活性	BMS-777607不太影响肿瘤细胞生长,在PC-3和DU145 细胞中,其对肝细胞生长因子诱导的细胞分散有抑制作用,其还剂量依赖性抑制细胞迁移和入侵（IC50<0.1 μM）。BMS-777607是选择性ATP竞争Met激酶抑制剂,对c-Met自磷酸化有较强抑制,对GTL-16细胞裂解物的IC50为20 nM,且对Met驱动的肿瘤细胞系如GTL-16细胞系,H1993和 U87细胞的增殖有选择性抑制作用。在DU145前列腺癌细胞中,BMS-777607对肝细胞生长因子 (HGF)引起的c-Met自磷酸化有抑制作用（IC50<1 nM）。BMS-777607（1 μM）处理24 h,有效抑制KHT细胞分散、活动和入侵,这与MET基因抑制相关,且对细胞增殖和集落形成有一定影响。在高度转移性鼠科KHT细胞中,BMS-777607（10 μM）处理2 h,有效清除自磷酸化的c-Met水平（IC50：10 nM）,不影响全部c-Met,从而剂量依赖性地抑制下游信号分子包括 ERK, Akt, p70S6K 和 S6。
存储条件	keep away from moisture,store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 44 mg/mL (85.8 mM)
关键字	c-Met/HGFR \| Inhibitor \| Mer \| inhibit \| Axl \| TAM Receptor \| BMS 777607 \| Tyro3 \| BMS-817378 \| BMS817378
相关产品	Capmatinib 2HCl \| Cabozantinib S-malate \| Crizotinib \| Gilteritinib \| NCT-503 \| (±)-Norcantharidin \| Sitravatinib \| Capmatinib xHCl \| L-Ascorbic acid 2-phosphate trisodium \| Bacitracin Zinc \| AMG-458 \| UNC2025
相关库	抗乳腺癌化合物库 \| 细胞因子抑制剂库 \| 抗结直肠癌化合物库 \| ReFRAME 相关化合物库 \| 激酶抑制剂库 \| 含氟化合物库 \| NO PAINS 化合物库 \| 抗肺癌化合物库 \| 酪氨酸激酶分子库 \| 细胞重编程化合物库

BMS-777607|||BMS777607|||BMS 817378|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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