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Ensartinib hydrochloride (X-396 dihydrochloride) 是双重的 ALK/MET 抑制剂,IC50分别 <0.4 nM 和 0.74 nM。
Ensartinib hydrochloride (X-396 dihydrochloride) 是双重的 ALK/MET 抑制剂,IC50分别 <0.4 nM 和 0.74 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 496 | 现货 | |
2 mg | ¥ 733 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,990 | 现货 | |
25 mg | ¥ 3,970 | 现货 | |
50 mg | ¥ 5,850 | 现货 | |
100 mg | ¥ 8,120 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,730 | 现货 |
产品描述 | Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM. |
靶点活性 | GOPC-ROS1:<1 nM, ALK (variants):<4 nM, ALK:<4 nM, TrkC:<1 nM, TPM3-TRKA:<1 nM |
体外活性 | Ensartinib potently inhibits both wild-type ALK and all evaluated ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM. Besides ALK, ensartinib also potently inhibits GOPC-ROS1, TPM3-TRKA, and TRKC with an IC50 of <1 nM, and inhibits EphA1, EphA2, EphB1 and c-MET with an IC50 of 1-10 nM[1]. |
别名 | X-396 dihydrochloride, Ensartinib dihydrochloride |
分子量 | 634.36 |
分子式 | C26H29Cl4FN6O3 |
CAS No. | 2137030-98-7 |
Smiles | Cl.Cl.C[C@@H](Oc1cc(nnc1N)C(=O)Nc1ccc(cc1)C(=O)N1C[C@H](C)N[C@H](C)C1)c1c(Cl)ccc(F)c1Cl |
密度 | no data available |
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: 33 mg/mL (52.02 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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