生物活性
Pelitinib (EKB-569)是一种有效的,不可逆EGFR抑制剂,IC50为38.5 nM
Targets
| Target | Value |
| EGFR | IC50: 38.5nM |
| Src | IC50: 282nM |
| MEK/ERK | IC50: 800nM |
| ErbB2 | IC50: 1.255μM |
| Raf | IC50: 3.353μM |
| c-Met | IC50: 4.1μM |
| CDK4 | IC50: >20μM |
化学数据
| 目录号 | A10706 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 467.9 |
| Formula | C24H23ClFN5O2 |
| 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. | 257933-82-7 |
| Synonyms | WAY-EKB 569 |
| SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)F)Cl)C#N)NC(=O)/C=C/CN(C)C |
溶解度
| In vitro | DMSO | 12 mg/mL (25.64 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<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 | 21.37 mL | 106.86 mL | 213.72 mL |
| 0.5 mM | 4.27 mL | 21.37 mL | 42.74 mL |
| 1 mM | 2.14 mL | 10.69 mL | 21.37 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.27 mL |
*The above data is based on the productmolecular weight 467.9 . 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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