Chemical Structure : DJX-A-KM
CAS No.:
DJX-A-KM
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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687.22
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Formula
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C36H40ClFN8O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Deng J, et al. Nat Commun. 2026 Mar 26. doi: 10.1038/s41467-026-71093-9.
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