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EGFR mutant-IN-1

  Cat. No.:  DC46219  
Chemical Structure
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More than 5000 active chemicals with high quality for research!
Field of application
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.:
Chemical Name: EGFR mutant-IN-1
SMILES: O=C1C(C2=CC=CC(F)=C2Cl)=C(C)C3=CN=C(NC4=CC=C(N5CCN(C)CC5)C(C)=C4)N=C3N1[C@H]6CN(C(CC)=O)CCC6
Formula: C34H39ClFN7O2
M.Wt: 632.17
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC47669 EGFR-IN-18 EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
DC47668 EGFR-IN-17 EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
DC47667 EGFR/CSC-IN-1 EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer treatment.
DC47271 Tyrphostin 8 Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
DC47115 Befotertinib Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
DC46929 Erlotinib-13C6 Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
DC46464 BGB-102 BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
DC46456 JNJ28871063 hydrochloride JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
DC46434 JBJ-02-112-05 JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.
DC46219 EGFR mutant-IN-1 EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).
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