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ALK-IN-1 (AP26113) 是一种高效的、选择性的 ALK 激酶抑制剂。
ALK-IN-1 (AP26113) 是一种高效的、选择性的 ALK 激酶抑制剂。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 187 | 现货 | |
2 mg | ¥ 259 | 现货 | |
5 mg | ¥ 413 | 现货 | |
10 mg | ¥ 662 | 现货 | |
25 mg | ¥ 987 | 现货 | |
50 mg | ¥ 1,490 | 现货 | |
100 mg | ¥ 2,480 | 现货 | |
200 mg | ¥ 3,660 | 现货 | |
500 mg | ¥ 5,860 | 现货 |
产品描述 | ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2. |
靶点活性 | ALK:0.62 nM |
体外活性 | 在HCC827(EGFR-DEL)或HCC827(EGFR-DEL/T790M)移植瘤小鼠模型中,AP26113(25 mg/kg),能够抑制肿瘤细胞生长.在Karpas-299移植瘤小鼠模型中,AP26113(<50 mg/kg)抑制p-ALK.在Karpas-299移植瘤小鼠模型和 H3122 移植瘤小鼠模型中,AP26113(<50 mg/kg)抑制肿瘤生长. |
体内活性 | 在SU-DHL-1(GI50=9 nM), H3122 (GI50=4 nM)和 Ba/F3-EML4-ALK v1(1 gI50=3 nM)细胞系中,抑制生长细胞生长。在表达EGFR-DEL(HCC827)的NSCLC细胞系中(IC50=62 nM),AP26113作用于抑制EGFR 磷酸化,抑制细胞生长。 |
细胞实验 | Three-day cell viability assays are carried out by plating 2,000, 1,500 and 2,000 cells per well of Ba/F3, PC9 or MGH121, respectively, into black transparent-bottom 96-well plates. On the same day for Ba/F3 cells and the following day for PC9 and MGH121 cells, the cells are treated with each TKI across a 10-dose range from 0.3 nM to 10 μM. After 72 h of drug treatment, cell viability is measured using the CellTiter-Glo assay. (Only for Reference) |
别名 | Brigatinib, AP26113-analog, AP26113 |
分子量 | 529.01 |
分子式 | C26H34ClN6O2P |
CAS No. | 1197958-12-5 |
Smiles | N(C1=C(P(C)(C)=O)C=CC=C1)C2=NC(NC3=C(OC)C=C(C=C3)N4CCC(N(C)C)CC4)=NC=C2Cl |
密度 | 1.29 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 | Ethanol: 98 mg/mL (185.3 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 1 mg/mL, Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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