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X-376 (Ensartinib) 是一种有效的ALK 抑制剂,对许多具有crizotinib 抗性的ALK 突变型和中枢神经系统转移具有高活性。它能有效地抑制野生型ALK 和ALK 变体(F1174, C1156Y, L1196M, S1206R, T1151和G1202R 突变型),IC50小于4 nM。
X-376 (Ensartinib) 是一种有效的ALK 抑制剂,对许多具有crizotinib 抗性的ALK 突变型和中枢神经系统转移具有高活性。它能有效地抑制野生型ALK 和ALK 变体(F1174, C1156Y, L1196M, S1206R, T1151和G1202R 突变型),IC50小于4 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 493 | 现货 | |
2 mg | ¥ 737 | 现货 | |
5 mg | ¥ 1,380 | 现货 | |
10 mg | ¥ 1,990 | 现货 | |
25 mg | ¥ 3,290 | 现货 | |
50 mg | ¥ 4,790 | 现货 | |
100 mg | ¥ 6,630 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,690 | 现货 |
产品描述 | X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins, and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. |
靶点活性 | ALK:0.61 nM, MET:0.69 nM |
体外活性 | Ensartinib是一种选择性ALK抑制剂,从临床活性和安全性两方面提供了有希望的优势[1]。 |
别名 | 恩沙替尼, X-396, Ensartinib |
分子量 | 547.41 |
分子式 | C25H25Cl2FN6O3 |
CAS No. | 1365267-27-1 |
Smiles | C[C@@H](Oc1cc(nnc1N)C(=O)Nc1ccc(cc1)C(=O)N1CCN(C)CC1)c1c(Cl)ccc(F)c1Cl |
密度 | 1.428 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 37 mg/mL (67.59 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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