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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-JND3229
JND3229

Chemical Structure : JND3229

CAS No.: 2260886-64-2

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JND3229 (JND-3229;JND 3229)

货号: 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.

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2 mg ￥1580 In stock
5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 617.195
分子式 C33H41ClN8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

1. Lu X, et al. ACS Med Chem Lett. 2018 Oct 8;9(11):1123-1127.

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