生物活性
Mubritinib (TAK 165)是一种有效的EGFR和p34cdc2抑制剂，IC50分别为6 nM和0.2 ?M。Mubritinib（TAK 165）也抑制p33cdk2和p33cdk5。
Targets
| Target | Value |
| HER2/ErbB2 | IC50: 6.0nM |
| EGFR | IC50: >25μM |
| FGFR | IC50: >25μM |
| PDGFR | IC50: >25μM |
| JAK1 | IC50: >25μM |
| Src | IC50: >25μM |
| BLK | IC50: >25μM |
化学数据
| 目录号 | A10612 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 468.5 |
| Formula | C25H23F3N4O2 |
| 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. | 366017-09-6 |
| Synonyms | TAK-165, TAK165 |
| SMILES | C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)/C=C/C4=CC=C(C=C4)C(F)(F)F |
溶解度
| In vitro (25°C) | DMSO | 12 mg/mL (25.61 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 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 | 21.34 mL | 106.72 mL | 213.45 mL |
| 0.5 mM | 4.27 mL | 21.34 mL | 42.69 mL |
| 1 mM | 2.13 mL | 10.67 mL | 21.34 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
*The above data is based on the productmolecular weight 468.5 . 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.
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