CAS |
184475-35-2 |
Chinese Name |
吉非替尼 |
English Name |
Gefitinib |
Synonym |
吉非替尼;SR-47436;BMS-186295;易瑞沙; |
Unit |
Bottle |
Purity |
HPLC≥98% |
Molecular Formula |
C22H24ClFN4O3 |
Molecular Weight |
446.9 |
Appearance |
White to off-white solid |
Storage |
Powder : 2-8℃, 2 years; In solvent(mother liquid): -20℃, 1 month; -80℃, 6 months |
Solubility |
Soluble in DMSO |
MDL |
MFCD04307832 |
EC |
EINECS 643-034-7 |
InChIKey |
XGALLCVXEZPNRQ-UHFFFAOYSA-N |
InChI |
InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27) |
PubChem CID |
123631 |
SMILES |
ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F |
Description |
It is an effective and selective EGFR tyrosine kinase inhibitor and can also induce autophagy. It has anti-tumor activity. |
Target Point |
EGFR |
Passage |
Angiogenesis;Protein Tyrosine Kinase/RTK; JAK/STAT Signaling |
Data Literature Source |
[1]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.
[2]. Moasser MM, et al. The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8.
[3]. Morgillo F, et al. Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19.
[4]. Miyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85.
[5]. Noh CK, et al. Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. J Sep Sci. 2017 Jul 27.
[6]. Dhar D, et al. Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. |
Specification |
10mg 10mM*1mL (in DMSO) 50mg |