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| Cas No.: | 879127-07-8 |
| Chemical Name: | N-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide |
| Synonyms: | EGFR inhibitor; EGFR-inhibitor; EGFRinhibitor; YUN27078; YUN-27078; YUN 27078; |
| SMILES: | O=C(C1CC1)NC2=CC=CC(NC3=NC=NC(NC4=CC=CC(C(F)(F)F)=C4)=C3)=C2 |
| Formula: | C21H18F3N5O |
| M.Wt: | 413.40 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | EGFR inhibitor(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]. |
| Target: | EGFR (WT):21 nM (IC50) EGFRL858R:63 nM (IC50) EGFRL861Q:4 nM (IC50) HER4:7640 nM (IC50) |
| In Vitro: | EGFR-IN-12 (EGFR inhibitor 324674; 0-2 µM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations[2]. EGFR-IN-12 (EGFR inhibitor 324674; 0-3 µM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner[2]. EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 µM and 1.04 µM, respectively[2]. Pretreatment of cells with EGFR-IN-12 (compound 1; 10 µM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12[1]. Apoptosis Analysis[1] Cell Line: HT29 and SW480 cells Concentration: 0 µM, 1 µM, 2 µM Incubation Time: 48 hours Result: Induced apoptosis in HT29 cells and SW480 cells. Western Blot Analysis[1] Cell Line: HT29 and SW480 cells Concentration: 0 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM Incubation Time: 3 hours Result: Inhibited EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner. |
| 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. |