生物活性
Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。
Targets
| Target | Value |
| c-Src | IC50: 2.7nM |
| LCK | IC50:<4nM |
| c-YES | IC50: 4nM |
| EGFR(L861Q) | IC50: 4nM |
| Lyn | IC50: 5nM |
| EGFR(L858R) | IC50: 5nM |
| Fyn | IC50: 10nM |
| FGR | IC50: 10nM |
| BLK | IC50: 11nM |
| v-Abl | IC50: 30nM |
| EGFR | IC50: 66nM |
| c-Kit | IC50: 200nM |
| EphA2 | IC50: 236nM |
| CSK | IC50: >1μM |
| PDGFRβ | IC50: >5μM |
| PDGFRα | IC50: 10μM |
| CDK2 | IC50: 10μM |
| VEGFR3/FLT4 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| MEK | IC50: 14μM |
| VEGFR2/KDR | IC50: 21μM |
| VEGFR1/FLT1 | IC50: >100μM |
化学数据
| 目录号 | A10108 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 542.0 |
| Formula | C27H32ClN5O5 |
| 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. | 379231-04-6 |
| Synonyms | AZD-0530 |
| SMILES | CN1CCN(CC1)CCOC2=CC(=C3C(=C2)N=CN=C3NC4=C(C=CC5=C4OCO5)Cl)OC6CCOCC6 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 34 mg/mL (62.73 mM) |
| Water | Insoluble |
| Ethanol | 30 mg/mL (55.35 mM) |
| In vivo | 2% DMSO+30% PEG 300+ddH2O | 4 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 18.45 mL | 92.25 mL | 184.5 mL |
| 0.5 mM | 3.69 mL | 18.45 mL | 36.9 mL |
| 1 mM | 1.85 mL | 9.23 mL | 18.45 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.69 mL |
*The above data is based on the productmolecular weight 542.0 . 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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