生物活性
IC-87114是首个同种型选择性PI3K抑制剂:p110M-NM-4(IC50 = 0.13 M-BM-5M)与p110M-NM-1(IC50 = 200 M-BM-5M)、p110M-NM-2(IC50 = 16 M-BM-5M)和p110M-NM-3(IC50 = 61 M-BM-5M)。
靶点信息
| PI3Kδ (Cell-free assay) | PI3Kγ (Cell-free assay) | PI3Kβ (Cell-free assay) | | |
| 0.5 μM | 29 μM | 75 μM | | |
化学数据
| 目录号 | A10463 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 397.4 |
| Formula | C22H19N7O |
| 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. | 371242-69-2 |
| SMILES | CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C=NC5=C4N=CN=C5N |
溶解度
| In vitro (25°C) | DMSO | 0.62 mg/mL (1.56 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+30% PEG 300+ddH2O | 0.6 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 | 25.16 mL | 125.82 mL | 251.64 mL |
| 0.5 mM | 5.03 mL | 25.16 mL | 50.33 mL |
| 1 mM | 2.52 mL | 12.58 mL | 25.16 mL |
| 5 mM | 0.5 mL | 2.52 mL | 5.03 mL |
*The above data is based on the productmolecular weight 397.4 . 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.
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