生物活性
CH5424802是一种有效的，选择性的，口服的ALK抑制剂，具有独特的化学支架，对具有ALK基因改变的癌症表现出优先的抗肿瘤活性。
Targets
| Target | Value |
| ALK(F1174L) | IC50: 1nM |
| ALK | IC50: 1.9nM |
| ALK(R1275Q) | IC50: 3.5nM |
| INSR | IC50: 550nM |
| KDR | IC50: 1.4μM |
| Abl | IC50: >5μM |
| EGFR | IC50: >5μM |
| FGFR2 | IC50: >5μM |
| HER2 | IC50: >5μM |
| IGF-1R | IC50: >5μM |
| JAK1 | IC50: >5μM |
| Kit | IC50: >5μM |
| Met | IC50: >5μM |
| PDGFRβ | IC50: >5μM |
| Src | IC50: >5μM |
| Akt1 | IC50: >5μM |
| Akt2 | IC50: >5μM |
| Akt3 | IC50: >5μM |
| AuroraA | IC50: >5μM |
| CDK1 | IC50: >5μM |
| CDK2 | IC50: >5μM |
| MEK1 | IC50: >5μM |
| PKA | IC50: >5μM |
| PKCα | IC50: >5μM |
| PKCβ1 | IC50: >5μM |
| PKCβ2 | IC50: >5μM |
| Raf-1 | IC50: >5μM |
化学数据
| 目录号 | A11134 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 482.6 |
| Formula | C30H34N4O2 |
| 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. | 1256580-46-7 |
| Synonyms | CH-5424802 |
| SMILES | CCC1=C(C=C2C(=C1)C(=O)C3=C(C2(C)C)NC4=C3C=CC(=C4)C#N)N5CCC(CC5)N6CCOCC6 |
溶解度
| In vitro | DMSO | Warmed: 0.5 mg/mL (1.03 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<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 | 20.72 mL | 103.61 mL | 207.21 mL |
| 0.5 mM | 4.14 mL | 20.72 mL | 41.44 mL |
| 1 mM | 2.07 mL | 10.36 mL | 20.72 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.14 mL |
*The above data is based on the productmolecular weight 482.6 . 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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