生物活性
WYE-354是一种有效的mTOR细胞渗透抑制剂（IC50 = 4.3 nM），可阻断通过mTOR复合体1（mTORC1）和mTORC2的信号传导。它是PI3Kα（IC50 = 1026 nM）和其他激酶的弱得多的抑制剂。
Targets
| Target | Value |
| mTOR | IC50: 5nM |
| PI3Kα | IC50: 1.89μM |
| PI3Kγ | IC50: 7.37μM |
| GCK | IC50: >50μM |
| Hck | IC50: >50μM |
| IKKα | IC50: >50μM |
| Lyn | IC50: >50μM |
| Met | IC50: >50μM |
| MK2 | IC50: >50μM |
| p38α | IC50: >50μM |
| PDGFRα | IC50: >50μM |
| PKA | IC50: >50μM |
| PKBα | IC50: >50μM |
| PKCα | IC50: >50μM |
| PKCβ | IC50: >50μM |
| ROCK1 | IC50: >50μM |
| RSK1 | IC50: >50μM |
| 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 |
化学数据
| 目录号 | A10989 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 495.5 |
| Formula | C24H29N7O5 |
| 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. | 1062169-56-5 |
| Synonyms | WYE354 |
| SMILES | COC(=O)NC1=CC=C(C=C1)C2=NC3=C(C=NN3C4CCN(CC4)C(=O)OC)C(=N2)N5CCOCC5 |
溶解度
| In vitro (25°C) | DMSO | 95 mg/mL (191.71 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+30% PEG 300+5% Tween 80+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 | 20.18 mL | 100.91 mL | 201.82 mL |
| 0.5 mM | 4.04 mL | 20.18 mL | 40.36 mL |
| 1 mM | 2.02 mL | 10.09 mL | 20.18 mL |
| 5 mM | 0.4 mL | 2.02 mL | 4.04 mL |
*The above data is based on the productmolecular weight 495.5 . 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.
