| 应用 |
An irreversible pan-erbB tyrosine kinase inhibitor. |
| 产品介绍 |
Canertinib (CI-1033)是一种pan-ErbB抑制剂，同时抑制EGFR和ErbB2，IC50分别为1.5 nM和9.0 nM，但对PDGFR， FGFR， InsR， PKC，和CDK1/2/4等均无抑制活性。 |
| 备注 |
Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3. |
| 生化机理 |
Canertinib is a potent and selective inhibitor of tyrosine residue phosphorylation of EGFR, blocking signal transgression and ceasing angiogenisis. Canertinib displays an IC50 = 1.5nM. Additionally, Canertinib’s action in inhibiting EGFR increases apoptosis in cancerous cell lines in a titratable fashion. |
| 别名 |
PD-183805;卡奈替尼; 卡耐替尼;N-[4-[(3-氯-4-氟苯基)氨基]-7-(3-吗啉-4-基丙氧基)喹唑啉-6-基]丙-2-烯酰胺;卡那替尼;;CI-1033;CI1033;CI 1033;PD183805;PD 183805;N-[4-(3-Chloro-4-fluoroanilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide |
