Chemical Structure : PLX-3618
CAS No.:
2851986-76-8
PLX-3618
(PLX3618)
Catalog No.: PC-22587Not For Human Use, Lab Use Only.
PLX-3618 is a potent, selective monovalent direct degrader of BRD4 (DC50=12.2 nM, HEK293T cells) that acts via the Recruitment of DCAF11, elicits UPS-mediated selective degradation of BRD4, resulting in potent antitumor activity in vitro and in vivo.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PLX-3618 is a potent, selective monovalent direct degrader of BRD4 (DC50=12.2 nM, HEK293T cells) that acts via the Recruitment of DCAF11, elicits UPS-mediated selective degradation of BRD4, resulting in potent antitumor activity in vitro and in vivo.
Like JQ1, PLX- 3618 exhibits selective bromodomain (BD) binding to the extra terminal (BET) family of proteins, with near equal potency to BD1 and BD2 of BRD4 with IC50 of 10 and 30 nM respectively.
PLX-3618 induces BRD4 degradation through the recruitment of DCAF11, requires ligand binding to both bromodomains.
PLX-3618 demonstrates potent and differential antitumor activity in vitro across 110 different solid and hematopoietic tumor cell lines.
PLX-3618 (5 mg/kg, 10 mg/kg, IP) elicits complete tumor regression in AML model.
Physicochemical Properties
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M.Wt
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601.69
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Formula
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C32H27N9O2S
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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)-[1,1'-biphenyl]-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
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References
1. Parker GS, et al. Mol Cancer Ther. 2024 Jun 22. doi: 10.1158/1535-7163.MCT-24-0219.
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