Chemical Structure : PLX-4104
CAS No.:
2851986-77-9
PLX-4104
(PLX4104)
Catalog No.: PC-26898Not For Human Use, Lab Use Only.
PLX-4104 is a potent, selective monovalent DCAF11-acting degrader of BRD4 with DC50 of 2 nM and Dmax of >95% in MV411 cells (24 h), shows antiproliferative activity with IC50 of 4 nM on MV-4-11 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PLX-4104 is a potent, selective monovalent DCAF11-acting degrader of BRD4 with DC50 of 2 nM and Dmax of >95% in MV411 cells (24 h), shows antiproliferative activity with IC50 of 4 nM on MV-4-11 cells.
PLX-4104 has IC50 of 4 nM in NanoBRET target engagement BET BRD assays.
PLX-4104 acts through the E3 ligase DCAF11.
PLX-4104 (2 and 6 mg/kg, PO) showed promising activity in vitro and complete tumor regression in NOD/SCID mice bearing MV-4-11 subcutaneous tumors.
Physicochemical Properties
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M.Wt
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619.68
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Formula
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C32H26FN9O2S
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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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(S)-N-(4'-(6-(2-amino-2-oxoethyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-4-fluoro-[1,1'-biphenyl]-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
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References
1. Leriche G, et al. ACS Med Chem Lett. 2026 Apr 6;17(5):1106-1113.
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