Product Description: EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity[1][2].
Applications: Cancer-Kinase/protease
Formula: C21H18F3N5O
References: [1]Qiong Zhang, et al. Discovery of EGFR Selective 4,6-disubstituted Pyrimidines From a Combinatorial Kinase-Directed Heterocycle Library. J Am Chem Soc. 2006 Feb 22;128(7):2182-3./[2]Zhiwei Yu, et al. Novel Irreversible EGFR Tyrosine Kinase Inhibitor 324674 Sensitizes Human Colon Carcinoma HT29 and SW480 Cells to Apoptosis by Blocking the EGFR Pathway. Biochem Biophys Res Commun. 2011 Aug 12;411(4):751-6.
CAS Number: 879127-07-8
Molecular Weight: 413.40
Compound Purity: 99.40
Research Area: Cancer
Solubility: DMSO : 250 mg/mL (ultrasonic)
Target: Apoptosis;EGFR
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