Gefitinib | 1589

Gefitinib was found to be a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM). The IC₅₀ values for Gefitinib to inhibit HT-29 and LoVo cell growth were 23.6 - >100 µM and 7.3 - 48.5 µM, respectively, when the exposure times are from 18 hours to 3 days. The IC₅₀ values of Gefitinib to the breast cancer cell lines BT20, HCC1937, MDA-MB-231, BT474, and SKBR3 are 15.5±1.4, 8.4±1.5, 20.7±1.1, 0.25±0.05, 0.88±0.31 µM, respectively

Gefitinib was found to be a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM).

1589 | Gefitinib DataSheet

Alternate Name/Synonyms: ZD-1839

Appearance: White to off-white solid

Formulation: N/A

CAS Number: 184475-35-2

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₂H₂₄ClFN₄O₃

Molecular Weight: 446.9

Cell-Permeable?: Yes

Purity: ≥99% by HPLC

Solubilities: DMSO (100 mg/ml)

Handling: Protect from light and moisture

Country of Origin: USA

Tag Line: An EGFR kinase inhibitor

MDL Number: MFCD04307832

PubChem CID: 123631

SMILES: COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

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)

InChi Key: XGALLCVXEZPNRQ-UHFFFAOYSA-N