Chemical Structure : 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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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.
| 分子量 | 687.22 | |
| 分子式 | C36H40ClFN8O3 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Deng J, et al. Nat Commun. 2026 Mar 26. doi: 10.1038/s41467-026-71093-9.
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