生物活性
Vistusertib (AZD2014)是一种新型mTOR抑制剂,无细胞试验中IC50为2.8 nM;对多种PI3K亚型(α/β/γ/δ)具有较高选择性。浓度为1 μM时,对大多数激酶无或有微弱结合力。
靶点信息
mTOR (Cell-free assay) | P-Akt (S473) (Cell-free assay) | pS6 (S235/236) (Cell-free assay) | | |
2.8 nM | 80 nM | 200 nM | | |
化学数据
目录号 | A11303 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 462.5 |
Formula | C25H30N6O3 |
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. | 1009298-59-2 |
Synonyms | AZD-2014 |
SMILES | C[C@H]1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOC[C@@H]5C |
溶解度
In vitro (25°C) | DMSO | 32 mg/mL (69.18 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 5% 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 | 21.62 mL | 108.11 mL | 216.22 mL |
0.5 mM | 4.32 mL | 21.62 mL | 43.24 mL |
1 mM | 2.16 mL | 10.81 mL | 21.62 mL |
5 mM | 0.43 mL | 2.16 mL | 4.32 mL |
*The above data is based on the productmolecular weight 462.5 . 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.