847949-49-9

847949-49-9 structure

Name: O-Desmethyl gefitinib
Chemical Name: 4-(3-chloro-4-fluoroanilino)-6-(3-morpholin-4-ylpropoxy)-1H-quinazolin-7-one
CAS Number: 847949-49-9
Molecular Formula: C₂₁H₂₂ClFN₄O₃
Molecular Weight: 432.87600
Catalog: Signaling Pathways JAK/STAT Signaling EGFR
Create Date: 2018-12-17 16:37:11
Modify Date: 2024-01-18 17:25:55
O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].

Name	4-(3-chloro-4-fluoroanilino)-6-(3-morpholin-4-ylpropoxy)-1H-quinazolin-7-one
Synonyms	7-Quinazolinol,4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy] O-Desmethyl Gefitinib O-Demethyl-Gefitinib 4-[(3-Chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol 4-(3'-chloro-4'-fluoroanilino)-7-hydroxy-6-(3-morpholinopropoxy)quinazoline Gefitinib Impurity 1

Description	O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> JAK/STAT Signaling >> EGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Target	IC50: 36 nM (EGFR)[2]
References	[1]. Kobayashi H, et al. Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinib. Med Oncol. 2016 Jun;33(6):57. [2]. McKillop D, et al. Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition. Xenobiotica. 2006 Jan;36(1):29-39.

HS Code	2934999090

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%