HKI-357
Cat. No.：YN340044
CAS No. ：848133-17-5
| 产品名称: | HKI-357 |
| CAS No.: | 848133-17-5 |
| Chemical Name: | (2E)-N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide |
| Synonyms: | HKI 357 |
| 分子量: | 574.05 |
| 分子式: | C₃₁H₂₉ClFN₅O₃ |
| SMILES: | O=C(NC1=C(OCC)C=C2N=CC(C#N)=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)C2=C1)/C=C/CN(C)C |
| 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: | HKI-357 是EGFR和ERBB2的不可逆双重抑制剂，IC50分别为 34 nM 和 33 nM。HKI-357 抑制 EGFR 自磷酸化 (检测位点为 Y1068)，及 AKT 和 MAPK 磷酸化。 |
| IC50和靶点: | [{name:"EGFR:34 nM (IC50)"},{name: "ErbB2:33 nM (IC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Tsou, H.-R., Overbeek-Klumpers, E.G., Hallett, W.A., et al.Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activityJ. Med. Chem.48(4),1107-1131(2005)
Kwak, E.L., Sordella, R., Bell, D.W., et al.Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinibProc. Natl. Acad. Sci. USA102(21),7665-7670(2005)
