LLC0424 | NSD2 degrader | Probechem Biochemicals

Chemical Structure : LLC0424

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LLC0424 (LLC-0424)

货号: 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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250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	823.86
分子式	C45H41N7O9
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-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

参考文献

1. Lianchao Liu, et al. J Med Chem. 2024 Apr 30. doi: 10.1021/acs.jmedchem.3c01765.

LLC0424 (LLC-0424)

生物&药学活性

物理化学性质&存储条件

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LLC0424 (LLC-0424)

生物&药学活性

物理化学性质&存储条件

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