生物活性
LDK-378是ALK(间变性淋巴瘤激酶)的高度选择性、生物利用度和AT竞争性小分子抑制剂，ALK是一种受体酪氨酸激酶，被认为是肺癌的重要药物靶点。
Targets
| Target | Value |
| ALK | IC50: 0.2nM |
| Insulin Receptor | IC50: 7nM |
| IGF-1R | IC50: 8nM |
| STK22D | IC50: 23nM |
| FLT3 | IC50: 60nM |
| FGFR2 | IC50: 0.26μM |
| RET | IC50: 0.4μM |
| FGFR3 | IC50: 0.43μM |
| LCK | IC50: 0.56μM |
| JAK2 | IC50: 0.61μM |
| AuroraA | IC50: 0.66μM |
| Lyn | IC50: 0.84μM |
| EGFR | IC50: 0.9μM |
| FGFR4 | IC50: 0.95μM |
| PDGFRα | IC50: 1.14μM |
| Abl | IC50: 1.25μM |
| ROCK2 | IC50: 1.27μM |
| c-Kit | IC50: 1.28μM |
| MKNK2 | IC50: 2.24μM |
| Syk | IC50: 3.05μM |
| c-Met | IC50: 3.17μM |
| BTK | IC50: 3.36μM |
| JAK1 | IC50: 3.73μM |
| CDK2 | IC50: 3.97μM |
| CDK4 | IC50: 4.72μM |
| ZAP70 | IC50: 9.7μM |
| Akt | IC50: >10μM |
| GSK-3α | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| PAK2 | IC50: >10μM |
化学数据
| 目录号 | A13238 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 558.14 |
| Formula | C28H36ClN5O3S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1032900-25-6 |
| Synonyms | LDK378,LDK 378 |
| SMILES | CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl |
溶解度
| In vitro | DMSO | Warmed: 18 mg/mL (32.25 mM) |
| Water | Insoluble |
| Ethanol | 3 mg/mL (5.37 mM) |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 17.92 mL | 89.58 mL | 179.17 mL |
| 0.5 mM | 3.58 mL | 17.92 mL | 35.83 mL |
| 1 mM | 1.79 mL | 8.96 mL | 17.92 mL |
| 5 mM | 0.36 mL | 1.79 mL | 3.58 mL |
*The above data is based on the productmolecular weight 558.14. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
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