应用 |
A Met inhibitor effective against various cell lines
Crizotinib has been used:
· to investigate its effects on hepatocyte growth factor receptor (c-Met) expression, proliferation and apoptosis
· to block neurotrophic tyrosine kinase receptor type 1 (NTRK1) activity in epithelial cells
· to restore sensitivity to erlotinib |
产品介绍 |
PF-2341066 shows inhibition of Met phosphorylation in mIMCD3 mouse of MDCK canine epithelial cells with an IC50 of 5 nM and 20 nM, respectively, as well as NCI-H69 and HOP92 cells, with an IC50 of 13 nM and 16 nM, respectively. PF-2341066 shows a near-equivalent IC50 of 24 nM against the nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) oncogenic fusion varient of the ALK RTK expressed by the KARPAS299 human anaplastic large-cell lymphoma (ALCL) cell line. PF-2341066 supresses human GTL-16 gastric carcinoma cell growth with an IC50 of 9.7 nM. PF-2341066 induces apoptosis in GTL-16 cells with an IC5050 of 30 nM. |
生化机理 |
克唑替尼(PF-02341066)是受体酪氨酸激酶。 |
别名 |
克里唑替尼;3-[(1R)-1-(2,6-二氯-3-氟苯基)乙氧基]-5-[1-(4-哌啶)-1H-吡唑-4-基]-2-吡啶胺;克唑替尼, (R)-3-[1-(2,6-二氯-3-氟 - 苯基)-乙氧基]-5-(1-哌啶-4-基-1H-吡唑-4-基)-吡啶-2-基胺
;Xalkori;(R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine;PF 2341066, PF-02341066, PF02341066 |