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Chemical Structure : LLC0424
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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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.
| M.Wt | 823.86 | |
| Formula | C45H41N7O9 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lianchao Liu, et al. J Med Chem. 2024 Apr 30. doi: 10.1021/acs.jmedchem.3c01765.
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