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WYE-687是雷帕霉素（mTOR）哺乳动物靶标的新型ATP竞争性和选择性抑制剂，IC50为7 nM；抑制mTORC1/pS6K(T389)和mTORC2/P-AKT(S473)，但不抑制P-AKT(T308)，作用于mTOR比作用于PI3Kα(>100倍)和PI3Kγ(>500倍)选择性高。
Targets
| Target | Value |
|---|---|
| mTOR | IC50: 7nM |
| PI3Kα | IC50: 0.81μM |
| PI3Kγ | IC50: 3.11μM |
| p38α | IC50: 28.9μM |
| Src | IC50: >50μM |
| VEGFR2 | IC50: >50μM |
| Abl1 | IC50: >50μM |
| AuroraB | IC50: >50μM |
| CDK1/CyclinB | IC50: >50μM |
| CDK2/CyclinA | IC50: >50μM |
| Chk1 | IC50: >50μM |
| ERK2 | IC50: >50μM |
| Fyn | IC50: >50μM |
| GCK | IC50: >50μM |
| Hck | IC50: >50μM |
| IKKα | IC50: >50μM |
| Lyn | IC50: >50μM |
| Met | IC50: >50μM |
| MK2 | IC50: >50μM |
| PDGFRα | IC50: >50μM |
| PKA | IC50: >50μM |
| PKBα | IC50: >50μM |
| PKCα | IC50: >50μM |
| PKCβ | IC50: >50μM |
| ROCK1 | IC50: >50μM |
| RSK1 | IC50: >50μM |
| In vitro | DMSO | 0.45 mg/mL (0.85 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. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 18.92 mL | 94.59 mL | 189.18 mL |
| 0.5 mM | 3.78 mL | 18.92 mL | 37.84 mL |
| 1 mM | 1.89 mL | 9.46 mL | 18.92 mL |
| 5 mM | 0.38 mL | 1.89 mL | 3.78 mL |
*The above data is based on the productmolecular weight 528.61. 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 | A11187 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 528.61 |
| Formula | C28H32N8O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 1062161-90-3 |
| Synonyms | WYE687 |
| SMILES | COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)CC5=CN=CC=C5)C(=N2)N6CCOCC6 |
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