生物活性
GDC-0980 (Apitolisib,RG7422)是一种有效的，I型PI3激酶和mTOR激酶抑制剂（TORC1/2），对于p110α，β，δ和γ的体外IC50为5、27、7和14 nM。
靶点信息
| p110α (Cell-free assay) | p110δ (Cell-free assay) | p110γ (Cell-free assay) | mTOR (Cell-free assay) | p110β (Cell-free assay) |
| 5 nM | 7 nM | 14 nM | 17 nM(Ki app) | 27 nM |
化学数据
| 目录号 | A11023 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 498.6 |
| Formula | C23H30N8O3S |
| 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. | 1032754-93-0 |
| Synonyms | GDC0980 |
| SMILES | CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)CN5CCN(CC5)C(=O)[C@H](C)O |
溶解度
| In vitro (25°C) | DMSO | 20 mg/mL (40.11 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 0.5% methylcellulose+0.2% 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 20.06 mL | 100.28 mL | 200.56 mL |
| 0.5 mM | 4.01 mL | 20.06 mL | 40.11 mL |
| 1 mM | 2.01 mL | 10.03 mL | 20.06 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.01 mL |
*The above data is based on the productmolecular weight 498.6 . 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.
