Structure information available on request
Chemical structureResearch use only
CAT. NO. DC12804Featured

JND3229

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TotalUS$750
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Product overview

Description & Application

JND3229 is a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy (IC50 = 5.8 nM).

ParameterValue
Chemical NameN-[4-[3-(2-Chlorophenyl)-7-[3-methyl-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyrimidin-1-yl]cyclohexyl]propanamide
CAS No.2260886-64-2
SynonymsJND3229;JND 3229;N-(trans-4-(3-(2-Chlorophenyl)-7-((3-methyl-4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)cyclohexyl)propionamide;N-[4-[3-(2-Chlorophenyl)-7-[3-methyl-4-(4-methylpiperazin-1-yl)anilino]-2-oxo-4H-pyrimido[4,5-d]pyri
FormulaC33H41ClN8O2
M.Wt617.184
SMILESClC1=C([H])C([H])=C([H])C([H])=C1N1C([H])([H])C2=C([H])N=C(N([H])C3C([H])=C([H])C(=C(C([H])([H])[H])C=3[H])N3C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C3([H])[H])N=C2N(C1=O)C1([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N([H])C(C([H])([
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

JND3229 is a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy (IC50 = 5.8 nM).

In Vitro

JND3229 (JND-3229) is a novel highly potent, reversible EGFR C797S mutant inhibitor, potently inhibits the kinase activities of EGFRL858R/T790M and EGFRL858R/T790M/C797 with IC50 of 5.8 nM and 30.5 nM, respectively; inhibits WT EGFR with IC50 of 6.8 nM, JND3229 potently inhibits the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in a dose-dependent manner in cell-based assays, also demonstrates strong inhibition on the EGFRC797S activation in the BaF3 cells; inhibits the proliferation of BaF3 cells harboring the EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S mutations with IC50 values of 0.51 and 0.32 μM, respectively; demonstrates in vivo monodrug anticancer efficacy in xenograft mouse models

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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