BMS-777607

别名: BMS 817378

BMS-777607 (BMS 817378)是一种Met相关的抑制剂,作用于c-MetAxlRonTyro3,在无细胞试验中IC50分别为3.9 nM,1.1 nM,1.8 nM和4.3 nM,作用于Met相关靶点比作用于Lck, VEGFR-2,和TrkA/B选择性高40倍,比作用于其他受体和非受体激酶选择性高500多倍。

BMS-777607 Chemical Structure

BMS-777607 Chemical Structure

CAS: 1025720-94-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2041.38 现货
5mg RMB 976.53 现货
50mg RMB 5498.71 现货
1g RMB 16134.3 现货
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客户使用Selleck的BMS-777607发表文献56

产品质控

批次: 纯度: 99.64%
99.14

BMS-777607相关产品

相关信号通路图

c-Met抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
T-47D Function assay 10 μM Induces polyploidy by 86 % 23468529
ZR-75-1 Growth inhibitory assay ~5 μM inhibits cell proliferation 23468529
T-47D Growth inhibitory assay ~5 μM inhibits cell proliferation 23468529
KHT Growth inhibitory assay ~10 μM inhibits KHT cell proliferation 22286523
KHT Function assay ~0.5 μM inhibits cell invasion 22286523
KHT Function assay ~0.5 μM inhibits cell migration 22286523
KHT Function assay ~1 μM prevents spontaneous KHT cell scattering with IC50 of 0.1-0.5 μM 22286523
PC-3 Growth inhibitory assay ~10 μM reduces cell proliferation 20515943
DU145 Function assay 0.1 μM impairs HGF-mediated cell invasion 20515943
PC-3 Function assay 0.1 μM impairs HGF-mediated cell invasion 20515943
DU145 Function assay 0.01 μM suppresses HGF-induced cell migration 20515943
PC-3 Function assay 0.01 μM suppresses HGF-induced cell migration 20515943
DU145 Function assay 0.1 μM exhibits inhibitory effect on HGF-induced cell scattering 20515943
PC-3 Function assay 0.1 μM exhibits inhibitory effect on HGF-induced cell scattering 20515943
ZR-75-1 Function assay 10 μM Induces polyploidy by 88% 23468529
T-47D Function assay 10 μM inhibits AURK-B function and induces its protein degradation 23468529
CHRF Function assay 10 μM inhibits cell division 25304900
HPDE Function assay 10 μM blocks constitutive activation and decreased AKT signaling 26477314
U118MG Kinase assay ~3 μM blocks AXL phosphorylation 26848524
SF126 Kinase assay ~3 μM blocks AXL phosphorylation 26848524
U118MG Cytoxicity assay 12.5 μM decreases glioma cell viability 26848524
SF126 Cytoxicity assay 12.5 μM decreases glioma cell viability 26848524
U118MG Apoptosis assay 12.5 μM induces glioma cell apoptosis 26848524
SF126 Apoptosis assay 12.5 μM induces glioma cell apoptosis 26848524
U118MG Function assay 12.5 μM blocks glioma cell migration and invasive growth pattern 26848524
SF126 Function assay 12.5 μM blocks glioma cell migration and invasive growth pattern 26848524
GTL16 Function assay 6.25 mg/kg Cmax in human GTL16 cells xenografted athymic mouse at 6.25 mg/kg, po, Cmax = 4.5 μM. 19260711
GTL16 Function assay 50 mg/kg Cmax in human GTL16 cells xenografted athymic mouse at 50 mg/kg, po, Cmax = 43.7 μM. 19260711
GTL16 Function assay 30 mins Inhibition of Met phosphorylation in human GTL16 cells after 30 mins, IC50 = 0.02 μM. 19260711
GTL16 Antiproliferative assay 72 hrs Antiproliferative activity against Met-dependent human GTL16 cells after 72 hrs by MTS assay, IC50 = 0.1 μM. 19260711
NCI-H1993 Antiproliferative assay 72 hrs Antiproliferative activity against Met-dependent human NCI-H1993 cells after 72 hrs by MTS assay, IC50 = 0.15 μM. 19260711
U87 Antiproliferative assay 72 hrs Antiproliferative activity against Met-driven human U87 cells after 72 hrs by MTS assay, IC50 = 0.16 μM. 19260711
BAF3 Cytotoxicity assay 72 hrs Cytotoxicity against mouse BAF3 cells expressing TPR-Met assessed as growth inhibition after 72 hrs, IC50 = 0.1884 μM. 24792774
DU145 Antiinvasive assay 1 hr Antiinvasive activity in human DU145 cells assessed as inhibition of HGF-induced cell motility preincubated for 1 hr before HGF treatment measured after 24 hrs by cell scattering assay, IC50 = 0.2 μM. 24900830
MKN45 Cytotoxicity assay 72 hrs Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs, IC50 = 0.2858 μM. 24792774
NCI-H1993 Cytotoxicity assay 48 hrs Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay, IC50 = 1.108 μM. 24900830
MGHU3 Antiproliferative assay 72 hrs Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay 30309671
RT112 Antiproliferative assay 72 hrs Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay 30309671
KHT Kinase assay blocks the c-Met signaling pathway with IC50 of 10 nM 22286523
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 BMS-777607 (BMS 817378)是一种Met相关的抑制剂,作用于c-MetAxlRonTyro3,在无细胞试验中IC50分别为3.9 nM,1.1 nM,1.8 nM和4.3 nM,作用于Met相关靶点比作用于Lck, VEGFR-2,和TrkA/B选择性高40倍,比作用于其他受体和非受体激酶选择性高500多倍。
特性 BMS 777607是有效的Met家族成员抑制剂,比作用于Lck, VEGFR-2,和TrkA/B的选择性高40多倍,比作用同样其他受体和非受体激酶选择性高500多倍。
靶点
Axl [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
Tyro3 [1]
(Cell-free assay)
Mer [1]
(Cell-free assay)
点击更多
1.1 nM 1.8 nM 3.9 nM 4.3 nM 14 nM
体外研究(In Vitro)
体外研究活性

BMS-777607是ATP竞争性Met激酶选择性抑制剂,有效抑制c-Met自磷酸化,作用于GTL-16细胞裂解物, IC50为20 nM,且选择性抑制Met驱动的肿瘤细胞系如GTL-16细胞系, H1993和 U87增殖。[1] BMS-777607 作用于DU145前列腺癌细胞,抑制肝细胞生长因子 (HGF)引起的c-Met自磷酸化, IC50<1 nM 。BMS 777607对肿瘤细胞生长作用效果不大,但是作用于PC-3 和DU145 细胞,抑制HGF诱导的细胞分散。BMS 777607作用于这两种细胞,也抑制刺激的细胞迁移和入侵,IC50<0.1 μM,这种作用存在剂量依赖性。[2] BMS 777607(~10 μM)作用于高度转移性鼠科KHT细胞2小时,有效清除自磷酸化的c-Met水平,IC50为10 nM,不影响全部 c-Met,导致下游信号分子包括 ERK, Akt, p70S6K 和 S6受抑制,这种作用存在剂量依赖性。纳摩尔级BMS-777607(~1 μM)处理24小时,有效抑制KHT细胞分散,活动,和入侵,这与MET基因抑制相关,适当影响细胞增殖和集落形成。[3]

细胞实验 细胞系 啮齿类纤维肉瘤KHT细胞
浓度 溶于DMSO,作为储存液(10 mM), 终浓度为10 μM 左右
孵育时间 2, 24和96小时
方法

用连续稀释的BMS 777607 处理KHT细胞96小时,然后进行MTT实验和台酚蓝排除,分别测定细胞增殖和细胞死亡。KHT细胞集落和BMS 777607温育24小时,然后用结晶紫(0.1%)染色,然后显影,测定细胞分散情况。使用无菌的1 ml吸管端在融合的KHT单层细胞上划2 mm 痕,随后用BMS-777607处理24小时,在4块随机区域中计数迁移到剥蚀地细胞数,用于测定细胞迁移情况。为了测定细胞入侵,用Matrigel预包被的转移嵌入板(8 μm 孔膜),和无血清培养基在有或无BMS 777607存在时,在37oC下温育2小时,使Matrigel再水化。悬浮在无血清培养基上的细胞装到小室顶端,悬浮在含10% FBS的完全培养基上的细胞装到小室底端,作为化学引诱物。温育24小时,移除 Matrigel,用结晶紫染色。显影并计数在滤液下面的入侵细胞。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-c-Met / c-Met / p-FAK / p-c-Src / p-Akt / p-S6K / p-S6 p53 / p21 / Survivin / p-Rb / Rb 22639908
Immunofluorescence α-tubulin / survivin 24444656
体内研究(In Vivo)
体内研究活性

BMS 777607按6.25-50 mg/kg剂量口服处理给药携带GTL-16人类移植瘤的无胸腺小鼠,明显降低肿瘤体积,且没有毒性。[1] BMS 777607按25 mg/kg剂量每天处理6-8周大的注射啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠,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,与对照组相比,没有明显毒性。BMS 777607按 10 mg/kg 低剂量处理,也适度但不显著抑制肺结节形成。[3]

动物实验 Animal Models 携带啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠
Dosages 10-25 mg/kg
Administration 饲喂处理,每天一次
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01721148 Completed
Malignant Solid Tumour
ASLAN Pharmaceuticals
October 2012 Phase 1
NCT00605618 Completed
Advanced Solid Tumors
Bristol-Myers Squibb
March 2008 Phase 1|Phase 2

化学信息&溶解度

分子量 512.89 分子式

C25H19ClF2N4O4

CAS号 1025720-94-8 SDF Download BMS-777607 SDF
Smiles CCOC1=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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 194.97 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
What formulation can we use to dissolve S1561 for mice in vivo study?

回答:
S1561 BMS-777607 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension. It is fine for oral gavage. If you are going to use it for injection, please try the following vehicle: 4% DMSO+30% PEG 300+ddH2O. BMS-777607 can be dissolved in it at 5 mg/ml as a clear solution.

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