Chemical Structure : LLC0424
CAS No.:
LLC0424
(LLC-0424)
Catalog No.: PC-22257Not For Human Use, Lab Use Only.
LLC0424 is a potent, selective, in vivo active NSD2 PROTAC degrader with DC50 of 20 nM, Dmax value of 96% in RPMI-8402 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
LLC0424 is a potent, selective, in vivo active NSD2 PROTAC degrader with DC50 of 20 nM, Dmax value of 96% in RPMI-8402 cells.
LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion, does not degrade NSD1 and NSD3 as well as CRBN neo-substrates IKZF1, IKZF3, GSPT1, and CK-1α.
LLC0424 causes continuous downregulation of H3K36me2 and growth inhibition of ALL cell lines with NSD2 mutation.
LLC0424 (60 mg/kg, i.p. or i.v.) showed potent NSD2 degradation in both the SEM and 22RV1 xenograft model.
Physicochemical Properties
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M.Wt
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823.86
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Formula
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C45H41N7O9
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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-Cyclopropyl-N-(4-((4-((1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)carbamoyl)phenyl)carbamoyl)benzyl)-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide
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References
1. Lianchao Liu, et al. J Med Chem. 2024 Apr 30. doi: 10.1021/acs.jmedchem.3c01765.
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