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DJX-A-KM

Chemical Structure : DJX-A-KM

CAS No.:

DJX-A-KM

货号: PC-26456Not For Human Use, Lab Use Only.

DJX-A-KM is a potent, selective FBXO28-recruiting degrader of KRASG12C with DC50 of 2 nM in NCI-H23 cells, Dmax=98%.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DJX-A-KM is a potent, selective FBXO28-recruiting degrader of KRASG12C with DC50 of 2 nM in NCI-H23 cells, Dmax=98%.
DJX-A-KM induces rapid and durable KRASG12C degradation via the ubiquitin–proteasome system, MLN4924 effectively prevents DJX-A-KM-induced KRASG12C degradation.
DJX-A-KM induces KRASG12C degradation by recruiting FBXO28. decreases p-ERK in a dose-dependent manner in NCI-H23 cells.
DJX-A-KM covalent modification of FBXO28 Cys98 to mediate KRASG12C degradation.
DJX-A-KM induces potent antitumor activity in a panel of KRASG12C mutant cell lines, including NCI-H23 and NCI-H358.
DJX-A-KM treatment resulted in dose-dependent tumor growth inhibition (TGI), achieving TGI values of 32%, 56%, and 83% at doses of 25 mg/kg, 50 mg/kg, and 100 mg/kg, respectively, in Ba/F3-KRASG12C xenograft model in BALB/c nude mice.

物理化学性质&存储条件

分子量 687.22
分子式 C36H40ClFN8O3
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-(2-((S)-2-(((7-(8-chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)ethyl)acrylamide

参考文献

1. Deng J, et al. Nat Commun. 2026 Mar 26. doi: 10.1038/s41467-026-71093-9.

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