EGFR-IN-12
Cat. No.：YN340199
| 产品名称: | EGFR-IN-12 |
| CAS No.: | 879127-07-8 |
| Chemical Name: | N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide |
| Synonyms: | EGFR Inhibitor |
| 分子量: | 413.40 |
| 分子式: | C₂₁H₁₈F₃N₅O |
| SMILES: | O=C(C1CC1)NC2=CC=CC(NC3=NC=NC(NC4=CC=CC(C(F)(F)F)=C4)=C3)=C2 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | EGFR-IN-12 是一种 4,6-二取代的嘧啶，是一种有效的，ATP 竞争性，不可逆且高度选择性的EGFR抑制剂，IC50为 21 nM。EGFR-IN-12 还抑制突变型EGFRL858R和EGFRL861Q，IC50分别为 63 nM 和 4 nM。EGFR-IN-12 对EGFR的选择性高于 HER4 (IC50= 7640 nM) 和 55种其他激酶。EGFR-IN-12 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。 |
| IC50和靶点: | [{name:"EGFR (WT):21 nM (IC50)"},{name: "EGFRL858R:63 nM (IC50)"},{name: "EGFRL861Q:4 nM (IC50)"},{name: "HER4:7640 nM (IC50)"}] |
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Zhang, Q., Liu, Y., Gao, F., et al.Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle libraryJ. Am. Chem. Soc.128(7),2182-2183(2006)
Ciardiello, F., and Tortora, G.EGFR antagonists in cancer treatmentN. Engl. J. Med.358(11),1160-1174(2008)
Okamoto, K., Okamoto, I., Okamoto, W., et al.Role of survivin in EGFR inhibitor-induced apoptosis in non-small cell lung cancers positive for EGFR mutationsCancer Res.70(24),10402-10410(2010)
