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TAS6417

  Cat. No.:  DC12161   Featured
Chemical Structure
1661854-97-2
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More than 5000 active chemicals with high quality for research!
Field of application
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1661854-97-2
Chemical Name: TAS-6417,TAS 6417,TAS6417
Synonyms: TAS-6417,TAS 6417,TAS6417
SMILES: NC1=C2C(N3C(C(C)=C[C@@H](C3)NC(C=C)=O)=C2C4=CC5=CC=CC=C5N=C4)=NC=N1
Formula: C23H20N6O
M.Wt: 396.44
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
In Vivo: TAS6417 causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues. TAS6417 prolongs survival of animals bearing lung cancer[1].
In Vitro: TAS6417 inhibits the in vitro phosphorylation activity of EGFR and its mutants including an exon 20 insertion mutation, with IC50 values ranging from 1.1±0.1 to 8.0±1.1 nM. TAS6417 suppresses the growth of cells expressing exon 20 insertion mutations of the EGFR gene, with a GI50 value of 86.5±28.5 nM for LXF 2478L cells and 45.4±2.6 nM for NCI-H1975 EGFR D770_N771insSVD cells. TAS6417 also potently inhibits proliferation in other cell lines harboring activating mutations or acquired resistance mutations, with mean GI50 values of 1.92±0.21 nM to 7.12±0.60 nM. In contrast, the effect of TAS6417 on cell proliferation in normal human epidermal keratinocytes (NHEK-Neo), of which WT EGFR is implicates in the growth and survival, is moderate[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70520 JBJ-09-063 JBJ-09-063 is a potent, mutant-selective allosteric EGFR inhibitor against EGFR L858R, T790M and C797S mutations, with IC50 of <0.1 nM for recombinant EGFR L858R/T790M kinase domain.
DC40932 JCN037 JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
DC7622 BIBX1382 BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
DC12161 TAS6417 TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM.
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DC5090 WZ4002 WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM; does not inhibit ERBB2 phosphorylation (T798I).
DC9775 WZ3146 WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
DC10519 SU 5214 SU 5214 is a modulator of tyrosine kinase signal transduction.
DC7078 AZD-8931(Sapitinib) Sapitinib(AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM respectively.
DC10479 RX518(CK-101:EGFR-IN-3) RX518(CK-101) is an orally available third-generation and selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations.
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