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AST-6是表皮生长因子受体1和2的新型不可逆抑制剂，可在体内外抑制肿瘤生长。
Targets
| Target | Value |
|---|---|
| EGFR | IC50: 0.5nM |
| ErbB4 | IC50: 0.8nM |
| ErbB2 | IC50: 3.0nM |
| EGFR(T790M/L858R) | IC50: 12nM |
| FLT1 | IC50: >10μM |
| KDR | IC50: >10μM |
| PDGFRα | IC50: >10μM |
| PDGFRβ | IC50: >10μM |
| c-Src | IC50: >10μM |
| c-Met | IC50: >10μM |
| c-Kit | IC50: >10μM |
| IGF-1R | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| RON | IC50: >10μM |
| Abl | IC50: >10μM |
| EphA2 | IC50: >10μM |
| EphB2 | IC50: >10μM |
| Tie-2 | IC50: >10μM |
| Syk | IC50: >10μM |
| PKCβ2 | IC50: >10μM |
| p70S6K | IC50: >10μM |
| JAK2 | IC50: >10μM |
| Pim2 | IC50: >10μM |
| Akt1 | IC50: >10μM |
| AuroraA | IC50: >10μM |
| CDK2 | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| In vitro (25°C) | DMSO | 115 mg/mL (185.16 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 0.5% hydroxyethyl cellulose | 28 mg/mL | |
|
* <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 | 16.1 mL | 80.5 mL | 161 mL |
| 0.5 mM | 3.22 mL | 16.1 mL | 32.2 mL |
| 1 mM | 1.61 mL | 8.05 mL | 16.1 mL |
| 5 mM | 0.32 mL | 1.61 mL | 3.22 mL |
*The above data is based on the productmolecular weight 621.1 . 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 | A10062 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 621.1 |
| Formula | C24H18ClFN4O2.C7H8O3S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 1050500-29-2 |
| Synonyms | AST6 |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)O.C=CC(=O)NC1=CC2=C(C=C1)N=CN=C2NC3=CC(=C(C=C3)OCC4=CC(=CC=C4)F)Cl |
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