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Chemical Structure : JND3229
CAS No.: 2260886-64-2
Catalog No.: PC-35826Not For Human Use, Lab Use Only.
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $158 | In stock | |
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
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| 100 mg | Get quote |
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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.
JND3229 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.
JND3229 also demonstrates strong inhibition on the EGFRC797S activation in the BaF3 cell.
JND3229 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.
JND3229 demonstrates in vivo monodrug anticancer efficacy in xenograft mouse models.
| M.Wt | 617.195 | |
| Formula | C33H41ClN8O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-((1r,4r)-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 |
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1. Lu X, et al. ACS Med Chem Lett. 2018 Oct 8;9(11):1123-1127.
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