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CAS No.: 2260886-64-2

JND3229 Catalog No. CSN24696

JND3229 is a new highly potent EGFR(C797S) inhibitor with IC50 values of 5.8nM, 30.5nM and 6.8nM for EGFR (L858R/T790M/C797S), EGFR (T790M, L858R) and EGFR, respectively.

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400-920-2911

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描述The epidermal growth factor receptor (EGFR) is one of the most validated molecular targets for anticancer drug discovery. Three generations of EGFR inhibitors have been approved by US FDA and achieved significantly clinical benefit in nonsmall cell lung cancer (NSCLC) patients ^[1]. JND3229 is a highly potent and fourth-generation EGFR^C797S reversible inhibitor with IC₅₀ value of 5.8 nM, and also potently suppressed EGFR^L858R/T790M and EGFR^WT with IC₅₀ values of 30.5 and 6.8 nM ^[1]. JND3229 potently inhibited the phosphorylation of EGFR^{L858R/T790M/C797S} and EGFR^{19D/T790M/C797S} in a dose-dependent manner. JND3229 potently inhibited the proliferation of BaF3 cells harboring the EGFR^{L858R/T790M/C797S} and EGFR^{19D/T790M/C797S} mutations with IC₅₀ values of 0.51 and 0.32 μM, respectively. JND3229 also obviously suppressed the proliferation of A431 cancer cells overexpressing EGFR^WT with an IC₅₀ value of 0.27 μM ^[1]. The in vivo anticancer efficacy of JND3229 was also examined using a xenograft mouse model. Administration of JND3229 caused an obvious suppression of tumor growth with a tumor growth inhibition (TGI) value of 42.2%. Further immunohistochemistry analysis demonstrated that JND3229 treatment significantly decreased the level of phosphorylated EGFR (p-EGFR) in the tumor tissues ^[1].
作用机制JND3229 was accommodated in the ATP binding site of the C797S-mutated EGFR with a reversible “U-shaped” configuration ^[1].
参考文献

[1] Lu X. 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6203 mL
- 8.1013 mL
- 16.2026 mL
- 5 mM
- 0.3241 mL
- 1.6203 mL
- 3.2405 mL
- 10 mM
- 0.1620 mL
- 0.8101 mL
- 1.6203 mL

技术信息

CAS号

2260886-64-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C33H41ClN8O2

运输

蓝冰

分子量

617.18

别名

溶解度

DMSO	95.0 mg/mL (153.9 mM) warming

动物实验配方

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