JND3229

For research use only. Not for therapeutic Use.

  • CAT Number: I019441
  • CAS Number: 2260886-64-2
  • Molecular Formula: C33H41ClN8O2
  • Molecular Weight: 617.18
  • Purity: ≥95%
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JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma[1].
JND3229 potently inhibits the proliferation of BaF3 cells (harboring the EGFRL858R/T790M/C797S and EGFR19D/T790M/C797Smutations), NCI-H1975 NSCLC cells (with EGFRT790M mutation) and A431 cancer cells (overexpressing EGFRWT) with IC50 values of 0.51, 0.32, 0.31 and 0.27 µM, respectively[1].
JND3229 (0.1, 0.3, 1, 3, 10 µM; 2 h) potently inhibits the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in engineering BaF3 cells[1].
JND3229 (10 mg/kg; i.p.; twice daily for 10 days) exhibits an obvious suppression of tumor growth, and shows target inhibition in vivo[1].


Catalog Number I019441
CAS Number 2260886-64-2
Synonyms

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

Molecular Formula C33H41ClN8O2
Purity ≥95%
InChI InChI=1S/C33H41ClN8O2/c1-4-30(43)36-24-9-12-26(13-10-24)42-31-23(21-41(33(42)44)29-8-6-5-7-27(29)34)20-35-32(38-31)37-25-11-14-28(22(2)19-25)40-17-15-39(3)16-18-40/h5-8,11,14,19-20,24,26H,4,9-10,12-13,15-18,21H2,1-3H3,(H,36,43)(H,35,37,38)
InChIKey WVLWGBZNXIVAKC-UHFFFAOYSA-N
SMILES CCC(=O)NC1CCC(CC1)N2C3=NC(=NC=C3CN(C2=O)C4=CC=CC=C4Cl)NC5=CC(=C(C=C5)N6CCN(CC6)C)C
Reference

[1]. Lu X, et al. Discovery of JND3229 as a New EGFRC797S Mutant Inhibitor with In Vivo Monodrug Efficacy. ACS Med Chem Lett. 2018 Oct 8;9(11):1123-1127.
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