JND3229

Cas No.:	2260886-64-2
Chemical Name:	N-[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
Synonyms:	JND3229;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
SMILES:	ClC1=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])([
Formula:	C33H41ClN8O2
M.Wt:	617.184
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

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