计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
BMS-777607, AXL 受体酪氨酸激酶抑制剂；巨噬细胞刺激 1 受体抑制剂；MER 原癌基因酪氨酸激酶抑制剂；MET 原癌基因受体酪氨酸激酶抑制剂；TYRO3 蛋白酪氨酸激酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BMS-777607 (BMS 817378)是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，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。
Information
BMS-777607 BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met , Axl , Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more th
In vitro
BMS-777607 is a selective ATP-competitive Met kinase inhibitor which potently blocks the autophosphorylation of c-Met with IC50 of 20 nM in GTL-16 cell lysates, and demonstrates selective inhibition of proliferation in Met-driven tumor cell lines, such as GTL-16 cell line, H1993 and U87. BMS-777607 inhibits hepatocyte growth factor (HGF)-triggered c-Met autophosphorylation with IC50 of <1 nM in PC-3 and DU145 prostate cancer cells. BMS 777607 has little effect on tumor cell growth, but exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells, with almost complete inhibition at 0.5 μM. BMS 777607 also suppresses stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 0.1 μM) in both cell lines. Application of BMS 777607 (~10 μM) to the highly metastatic murine KHT cells for 2 hours potently eliminates basal levels of autophosphorylated c-Met with IC50 of 10 nM without affecting the total c-Met, leading to dose-dependent inhibition of phosphorylation of downstream signaling molecules including ERK, Akt, p70S6K and S6. Treatment with BMS-777607 (~1 μM) for 24 hours potently inhibits the KHT cell scatter, motility and invasion at doses in the nanomolar range which consists with MET gene knockdown, and modestly affects cell proliferation and colony formation.
In vivo
Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity. Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control.
Cell Data
cell lines：PC12
Concentrations：Dissolved in DMSO as a stock solution (10 mM), final concentration ~10 μM.
Incubation Time：2, 24 and 96 hours
Powder Purity:≥98%
规格
英文别名
BMS 817378 | N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
BMS-777607
生化机理
BMS-777607 (BMS 817378) 是一种 Met 相关抑制剂，可抑制 c-Met、Axl、Ron 和 Tyro3，在无细胞实验中的 IC50 分别为 3.9 nM、1.1 nM、1.8 nM 和 4.3 nM，对 Met 相关靶点的选择性比 Lck、VEGFR-2 和 TrkA/B 高 40 倍，对所有其他受体和非受体激酶的选择性高 500 倍以上。1/2阶段。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
AXL 受体酪氨酸激酶抑制剂；巨噬细胞刺激 1 受体抑制剂；MER 原癌基因酪氨酸激酶抑制剂；MET 原癌基因受体酪氨酸激酶抑制剂；TYRO3 蛋白酪氨酸激酶抑制剂
名称和识别符
EC号
110-725-5
分子类型
小分子
Isomeric 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
MeSH Entry Terms
BMS 777607;BMS-777607;BMS777607;N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
分子量
512.89
Reaxy-Rn
18315448
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18315448&ln=
技术文档
高级数据
产品属性
| ALogP | 4 |
|---|
关联靶点（人）
MST1R
Tchem
巨噬细胞刺激蛋白受体(Macrophage-stimulating protein receptor)
(3 活性数据)
TYRO3
Tchem
酪氨酸蛋白激酶受体 TYRO3(Tyrosine-protein kinase receptor TYRO3)
(2 活性数据)
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(2 活性数据)
MET
Tclin
肝细胞生长因子受体(Hepatocyte growth factor receptor)
(14 活性数据)
MERTK
Tchem
酪氨酸蛋白激酶(Tyrosine-protein kinase Mer)
(3 活性数据)
PDGFRA
Tclin
血小板衍生生长因子受体α(Platelet-derived growth factor receptor alpha)
(1 活性数据)
AXL
Tchem
酪氨酸蛋白激酶受体UFO(Tyrosine-protein kinase receptor UFO)
(4 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2214592 |
分析证书 | B408833 |
溶液计算器
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