生物活性
SGI-1776 (free base)是Pim1的一种新型ATP竞争性抑制剂，在无细胞试验中的IC50为7 nM，选择性是Pim2和Pim3的50倍和10倍，对Flt3和haspin也有效。阶段1。
化学数据
| 目录号 | A10838 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 405.4 |
| Formula | C20H22F3N5O |
| 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. | 1025065-69-3 |
| Synonyms | SGI1776 |
| SMILES | CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2 |
溶解度
| In vitro (25°C) | DMSO | 70 mg/mL (172.66 mM) |
| Water | Insoluble |
| Ethanol | 70 mg/mL (172.66 mM) |
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 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 | 24.67 mL | 123.33 mL | 246.67 mL |
| 0.5 mM | 4.93 mL | 24.67 mL | 49.33 mL |
| 1 mM | 2.47 mL | 12.33 mL | 24.67 mL |
| 5 mM | 0.49 mL | 2.47 mL | 4.93 mL |
*The above data is based on the productmolecular weight 405.4 . 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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