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EAI045

CAS No. : 1942114-09-1

MCE 站：EAI045

产品活性：EAI045是突变体 EGFR 的第四代变构抑制剂，在10 μM ATP时抑制EGFR，EGFR^L858R，EGFR^T790M 和 EGFR^L858R/T790M 的IC₅₀ 值分别为1.9，0.019，0.19 和 0.002 μM。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: EAI045 potently inhibits EGFR Y1173 phosphorylation in H1975 cells (EC₅₀=2 nM), but not in HaCaT cells. EAI045 is an inhibitor of the L858R/T790M mutant with 1000-fold selectivity versus wild type EGFR at 1 mM ATP. Profiling of EAI045 against a panel of 250 protein kinases reveals exquisite selectivity; no other kinases are inhibited by more than 20% at 1 μM EAI045. EAI045 has high potency ａnd selectivity for L858R/T790M mutation. In L858R/T790M-mutant NSCLC cell line H1975 cells, EAI045 decreases but does not completely abolish the EGFR autophosphorylation. In stably transfected NIH-3T3 cells harboring the L858R/T790M EGFR mutant, EAI045 shows the same activity. In L858R-mutant H3255 cells, EAI045 exhibits moderate activity. In the HaCaT cells, a keratinocyte cell line with wild-type EGFR, EAI045 does not show any activity of inhibiting EGFR phosphorylation. It confirms the selectivity of EAI045 for mutant EGFR.

In Vivo: In a genetically engineered mouse model of L858R/T790Mmutant-driven lung cancer , remarkable tumor regression is observed in L858R/T790M-mutant mice treated with the combination of EAI045 ａnd cetuximab. No response is seen in those mice treated with EAI045 alone. The same effect is seen in both L858R/T790M/C797S- engineered Ba/F3 cells ａnd in mice carrying the L858R/T790M/C797S tumor xenografts. These assays clearly show that EAI045 can overcome resistance from acquired T790M ａnd C797S mutations.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Differentiation Inducing Compound Library  |  Anti-Hepatitis C Virus Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Gefitinib  |  Trastuzumab  |  Erlotinib  |  Cetuximab  |  AG490  |  Genistein  |  AG-1478  |  Pertuzumab  |  BI-4020  |  NSC 228155  |  Pelitinib  |  Mubritinib  |  TX1-85-1  |  Canertinib  |  Butein  |  PD168393  |  Daphnetin  |  AEE788  |  EGFR-IN-7  |  PD153035  |  Chrysophanol  |  Tyrphostin 23  |  BMS-599626 Hydrochloride  |  Lavendustin A  |  Trastuzumab emtansine  |  AV-412  |  Falnidamol

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