| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B408833-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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 |
| 产品介绍 |
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 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 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% |
| ALogP | 4 |
|---|
| 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 |
| 关联CAS | 1025720-94-8，1196681-44-3 |
| 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= |
首页
400-620-6333
