| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M409057-1ml |
1ml |
现货  |
|
| 英文别名 | (E)-1-(4-(4-((2-(4-(trifluoromethyl)styryl)oxazol-4-yl)methoxy)phenyl)butyl)-1H-1,2,3-triazole |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Mubritinib (TAK 165) |
| 生化机理 | Mubritinib (TAK-165) 是一种强效的 HER2/ErbB2 抑制剂，对 BT-474 细胞的 IC50 值为 6 nM；对 BT-474 细胞株中的 EGFR、FGFR、PDGFR、JAK1、Src 和 Blk 无活性。第 1 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 | 受体蛋白-酪氨酸激酶 erbB-2 抑制剂 |
| 产品介绍 |
Mubritinib (TAK 165)是一种有效的HER2/ErbB2抑制剂，IC50为6 nM；对EGFR， FGFR， PDGFR， JAK1， Src和Blk没有抑制活性。A selective, potent, and irreversible ErbB2 and EGFR inhibitor. Information Mubritinib (TAK 165) Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cell; no activity to EGFR, FGFR, PDGFR, JAK1, Src and Blk in BT-474 cell line. Phase 1. Mubritinib displays > 4000-fold selectivity over other tyrosine kinases, such as EGFR, FGFR, PDGFR, Jak1, Src and Blk. Mubritinib even at low concentration of 0.1 μM significantly blocks HER2 phosphorylation, leading to the downregulation of PI3K-Akt and MAPK pathway in cell line BT474 with high level of HER2. Mubritinib not only exhibits highly potent antiproliferative effect in ErbB2-overexpressing cancer cell line BT474 with an IC50 of 5 nM, but also displays marked antiproliferative effects in cell lines with HER2 expressed weakly with IC50 of 53 nM, 90 nM and 91 nM for LNCaP, LN-REC4 and T24, respectively. Mubritinib displays no inhibitory activities against PC-3 cells with HER2 expressed very faintly with IC50 of 4.62 μM, as well as EGFR-overexpressing HT1376 and ACHN cell lines with IC50 of >25 μM. In vivo Mubritinib significantly inhibits LN-REC4 xenograft with treatment/control tumor volume ratio of 26.5%. Although ineffective to inhibit the growth of UMUC-3 and ACHN cells in vitro (IC50s of 1.812 and >25 μM, respectively), oral administration of Mubritinib (10 or 20 mg/kg per day) significantly inhibits the growth of UMUC-3 and ACHN xenografts with treatment/control tumor volume ratio of 22.9% and 26%, respectively, as compared with Herceptin (20 mg/kg) which is ineffective to UMUC-3 tumor growth. cell lines： Concentrations：Dissolved in DMSO, final concentrations ~50 mM Incubation Time：72 hours Powder Purity:≥99% |
| ALogP | 5.4 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)/C=C/C4=CC=C(C=C4)C(F)(F)F |
| 分子量 | 468.47 |
| Reaxy-Rn | 12210978 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12210978&ln= |
| 熔点 | 154-166oC |
|---|
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