| CAS NO: | 879127-07-8 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 413.4 |
| Cas No. | 879127-07-8 |
| Formula | C21H18F3N5O |
| Synonyms | Epidermal Growth Factor Receptor Inhibitor |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥60.7 mg/mL in DMSO |
| Chemical Name | N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide |
| Canonical SMILES | O=C(C1CC1)NC2=CC=CC(NC3=CC(NC4=CC(C(F)(F)F)=CC=C4)=NC=N3)=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
EGFR inhibitor is a cell permeable, pyrimidine compound that selectively inhibits the EGFR kinase with IC50 value of 21 nM [1].
EGFR is a transmembrane protein, and is a receptor for members of epidermal growth factor family. The binding of EGFR with its ligands induces receptor dimerization and tyrosine autophosphorylation, and leads to cell proliferation. The overactivity of EGFR tyrosine kinases is associated with a number of cancers, inhibition of EGFR can downregulate antiapoptotic proteins such as surviving and upregulate proapoptotic proteins such as Bim. Thus, EGFR inhibitor can induce cell apoptosis, resulting in anti-tumor effectivity [2].
EGFR inhibitor inhibited EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR inhibitor also inhibited L858R and L861Q EGFR mutants with IC50 values of 63 and 4 nM, respectively [1].
References:
1. Q. Zhang, Y. Liu, F. Gao, et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. Journal of the American Chemical Society 128(7), 2182-2183 (2006).
2. F. Ciardiello, G. Tortora. EGFR antagonists in cancer treatment. New England Journal of Medicine 358(11), 1160-1174 (2008).
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