生物活性
PF299804是一种有效的,可口服的酪氨酸激酶人表皮生长因子受体(HER)1(EGFR),HER2和HER4不可逆抑制剂。
靶点信息
EGFR (Cell-free assay) | ErbB2 (Cell-free assay) | ErbB4 (Cell-free assay) | | |
6.0 nM | 45.7 nM | 73.7 nM | | |
化学数据
目录号 | A11051 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 469.9 |
Formula | C24H25ClFN5O2 |
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. | 1110813-31-4 |
Synonyms | PF-299804, Dacomitinib, PF-299 |
SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4 |
溶解度
In vitro (25°C) | DMSO | 17 mg/mL (36.17 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80, pH 9 | 9 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 | 21.28 mL | 106.41 mL | 212.81 mL |
0.5 mM | 4.26 mL | 21.28 mL | 42.56 mL |
1 mM | 2.13 mL | 10.64 mL | 21.28 mL |
5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
*The above data is based on the productmolecular weight 469.9 . 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.