| Identification | Back Directory | [Name]
JND3229 | [CAS]
2260886-64-2 | [Synonyms]
JND3229
JND3229
(JND-3229
JND3229;JND-3229;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
Propanamide, N-[trans-4-[3-(2-chlorophenyl)-3,4-dihydro-7-[[3-methyl-4-(4-methyl-1-piperazinyl)phenyl]amino]-2-oxopyrimido[4,5-d]pyrimidin-1(2H)-yl]cyclohexyl]- | [Molecular Formula]
C33H41ClN8O2 | [MDL Number]
MFCD32644591 | [MOL File]
2260886-64-2.mol | [Molecular Weight]
617.18 |
| Chemical Properties | Back Directory | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO : 12.5 mg/mL (20.25 mM; Need ultrasonic) | [form ]
Solid | [pka]
16.01±0.40(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | Animal Model: | BALB/c mice (bearing established BaF3-EGFR19D/T790M/C797S mouse xenograft tumors model)[1]. | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; twice daily for 10 days. | | Result: | Caused an obvious suppression of tumor growth with a Tumor Growth Inhibition (TGI) value of 42.2%.
Showed well tolerance without obvious body weight loss or other obvious toxic sign in the treated animals.
Significantly decreased the level of phosphorylated EGFR (p-EGFR) tin the tumor tissues.
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| [storage]
4°C, stored under nitrogen | [References]
[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. DOI:10.1021/acsmedchemlett.8b00373 |
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