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OSI-027是一种有效的，选择性的，可口服生物利用的mTOR激酶抑制剂，可抑制与mTOR的TORC1和TORC2复合物相关的激酶活性。
Targets
| Target | Value |
|---|---|
| mTOR | IC50: 4nM |
| mTORC1 | IC50: 22nM |
| mTORC2 | IC50: 65nM |
| PI3Kγ | IC50: 0.42μM |
| DNA-PK | IC50: 1.0μM |
| PI3Kα | IC50: 1.3μM |
| C-Raf | IC50: 1.6μM |
| YES1 | IC50: 2.8μM |
| EphA2 | IC50: 4.5μM |
| BTK | IC50: 5.0μM |
| LCK | IC50: 9.5μM |
| ACK1 | IC50: >10μM |
| p38α | IC50: 10.6μM |
| KDR | IC50: 19.0μM |
| PI3Kβ | IC50: >30μM |
| IGF-1R | IC50: >30μM |
| Insulin Receptor | IC50: >30μM |
| PDK-1 | IC50: >30μM |
| PKA | IC50: >30μM |
| EGFR/ErbB1 | IC50: >30μM |
| MST1R | IC50: >30μM |
| Src | IC50: >30μM |
| MEK1 | IC50: >30μM |
| Fyn | IC50: >30μM |
| In vitro (25°C) | DMSO | 16 mg/mL (39.36 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 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 | 24.61 mL | 123.03 mL | 246.06 mL |
| 0.5 mM | 4.92 mL | 24.61 mL | 49.21 mL |
| 1 mM | 2.46 mL | 12.3 mL | 24.61 mL |
| 5 mM | 0.49 mL | 2.46 mL | 4.92 mL |
*The above data is based on the productmolecular weight 406.4 . 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 | A11056 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 406.4 |
| Formula | C21H22N6O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 936890-98-1 |
| Synonyms | OSI027 |
| SMILES | COC1=CC=CC2=C/C(=C/3\C4=C(N=CNN4C(=N3)C5CCC(CC5)C(=O)O)N)/N=C21 |
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