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XMD8-87 (ACK1-B19)是TNK2抑制剂,对于D163E 和R806Q 突变体的IC50值分别为38和113 nM。
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XMD8-87 (ACK1-B19)是TNK2抑制剂,对于D163E 和R806Q 突变体的IC50值分别为38和113 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 289 | 现货 | |
5 mg | ¥ 668 | 现货 | |
10 mg | ¥ 1,150 | 现货 | |
25 mg | ¥ 2,570 | 现货 | |
50 mg | ¥ 3,780 | 现货 | |
100 mg | ¥ 5,390 | 现货 | |
200 mg | ¥ 7,360 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 738 | 现货 |
产品描述 | XMD8-87 (ACK1-B19) is a TNK2 inhibitor with activity in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types. |
靶点活性 | R806Q mutations:77 nM, D163E mutations:16nM |
体外活性 | XMD8-87 在抑制TNK2磷酸化方面显示出高效能。XMD8-87 和 XMD16-5 强效抑制在实体肿瘤类型中发现的TNK2截断突变的磷酸化。 |
激酶实验 | Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD8-87) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1]. |
细胞实验 | 293T cells expressing TNK2 are plated in 6-well format at a density of 250,000 cells per well 48 hours prior to treatment. Cells are then treated with a 100 μL of XMD8-87 or XMD16-5 at 5 μmol/L and with 9 1:1 serial dilutions down to ≈10 nmol/L. Two additional samples are treated with DMSO only. Cells are then incubated for 6 hours at 37°C. Protein extraction is accomplished by adding 300 μL of lysis buffer to cells after removing media. Plates are gently shaken for 5 minutes at room temperature. Lysates are collected and cleared of incompletely solubilized material by spinning for 10 minutes at maximum speed in a microcentrifuge. Samples are prepared for SDS-PAGE using the EPage loading buffer.(Only for Reference) |
别名 | ACK1-B19 |
分子量 | 445.52 |
分子式 | C24H27N7O2 |
CAS No. | 1234480-46-6 |
Smiles | COc1cc(ccc1Nc1ncc2NC(=O)c3ccccc3N(C)c2n1)N1CCN(C)CC1 |
密度 | 1.283 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: 5.33 mg/mL (11.97 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 5 mg/mL (11.2 mM) | ||||||||||||||||||||
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