PF-6274484 是一种有效的 EGFR 抑制剂，对 EGFR-L858R/T790M 和 WT EGFR 的 Kis 分别为 0.14 nM 和 0.18 nM。 PF-6274484 抑制 H1975 肿瘤细胞中的 EGFR-L858R/T790M 自磷酸化和 A549 肿瘤细胞中的 EGFR WT，IC50 分别为 6.6 和 5.8 nM。
| Cas No. | 1035638-91-5 |
| Canonical SMILES | FC1=C(Cl)C=C(NC2=NC=NC3=C2C=C(NC(C=C)=O)C(OC)=C3)C=C1 |
| 分子式 | C18H14ClFN4O2 |
| 分子量 | 372.8 |
| 溶解度 | DMF: 33 mg/ml,DMSO: 25 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PF-6274484 is an inhibitor of the EGF receptor (EGFR; IC50s = 0.18 and 0.14 nM for wild-type EGFR and inhibitor-resistant EGFRL858R/T790M, respectively). It inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells (IC50s = 5.8 and 6.6 nM, respectively). |
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