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XMD16-5 是TNK2抑制剂,对D163E 和R806Q 突变体的IC50值分别为16和77nM。
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XMD16-5 是TNK2抑制剂,对D163E 和R806Q 突变体的IC50值分别为16和77nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 363 | 现货 | |
2 mg | ¥ 532 | 现货 | |
5 mg | ¥ 877 | 现货 | |
10 mg | ¥ 1,450 | 现货 | |
25 mg | ¥ 2,350 | 现货 | |
50 mg | ¥ 3,480 | 现货 | |
100 mg | ¥ 4,970 | 现货 | |
500 mg | ¥ 10,600 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 983 | 现货 |
产品描述 | XMD16-5 is a TNK2 inhibitor. TNK2 genomic amplification has been associated with late-stage or metastatic lung and prostate Ys. Overexpression of TNK2 promoted metastasis in a mouse model of breast Y. TNK2 signaling is disrupted in breast, prostate and gastrointestinal tumors. |
靶点活性 | R806Q:77 nM, D163E:16nM |
体外活性 | XMD16-5在抑制TNK2磷酸化方面表现出强效。XMD8-87与XMD16-5能强力抑制在实体瘤类型中发现的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 (XMD16-5) 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) |
分子量 | 416.48 |
分子式 | C23H24N6O2 |
CAS No. | 1345098-78-3 |
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: 45 mg/mL (108.05 mM), Sonication is recommended. H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 5 mg/mL (12.01 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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