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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 |
| 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. |
|||
| 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.
| 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. |
| 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 |
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