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JND3229 Sale

目录号 : GC65436

JND3229 is a potent reversible inhibitor of EGFRC797S with an IC50 value of 5.8 nM. JND3229 also potently suppresses EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 nM and 6.8 nM, respectively.

JND3229 Chemical Structure

Cas No.:2260886-64-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥4,824.00
现货
5mg
¥3,555.00
现货
10mg
¥5,445.00
现货
50mg
¥16,650.00
现货
100mg
¥25,200.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

JND3229 is a potent reversible inhibitor of EGFRC797S with an IC50 value of 5.8 nM. JND3229 also potently suppresses EGFRL858R/T790M and EGFRWT with IC50 values of 30.5 nM and 6.8 nM, respectively.

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

Chemical Properties

Cas No. 2260886-64-2 SDF Download SDF
分子式 C33H41ClN8O2 分子量 617.18
溶解度 DMSO : 12.5 mg/mL (20.25 mM; Need ultrasonic) 储存条件 4°C, stored under nitrogen
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6203 mL 8.1014 mL 16.2027 mL
5 mM 0.3241 mL 1.6203 mL 3.2405 mL
10 mM 0.162 mL 0.8101 mL 1.6203 mL
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Research Update

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.PMID:30429956DOI:10.1021/acsmedchemlett.8b00373.

EGFRC797S mutation inducing resistance against third generation EGFR inhibitor drugs is an emerging "unmet clinical need" for nonsmall cell lung cancer patients. The pyrimidopyrimidinone derivative JND3229 was identified as a new highly potent EGFRC797S inhibitor with single digit nM potency. It also exhibited good in vitro and in vivo monodrug anticancer efficacy in a xenograft mouse model of BaF3/EGFR19D/T790M/C797S cells. A high-resolution X-ray crystallographic structure was also determined to elucidate the interactions between JND3229 and EGFRT790M/C797S. Our study provides an important structural and chemical basis for future development of new generation EGFRC797S inhibitors as anticancer drugs.