Chemical Structure : PRT3789
CAS No.:
2755761-78-3
PRT3789
(PRT-3789)
Catalog No.: PC-24667Not For Human Use, Lab Use Only.
PRT3789 is a first-in-class potent and selective SMARCA2 (BRM) degrader with DC50 of 0.72 nM in Hela cells, effectively catalyze the polyubiquitination of specific lysine residues of SMARCA2, resulting in SMARCA2 selective degradation over SMARCA4.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PRT3789 is a first-in-class potent and selective SMARCA2 (BRM) degrader with DC50 of 0.72 nM in Hela cells, effectively catalyze the polyubiquitination of specific lysine residues of SMARCA2, resulting in SMARCA2 selective degradation over SMARCA4.
PRT3789 selectively inhibits cell proliferation of SMARCA4-deficient cancer cells, but not SMARCA4 WT cells, when tested in a panel of cancer cell lines.
PRT3789 induces SMARCA4-deleted cancer cells to G1 cell-cycle arrest and apoptosis.
PRT3789 administration significantly inhibits the growth of SMARCA4-deleted NSCLC but demonstrates no effects on SMARCA4 WT tumor growth.
Physicochemical Properties
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M.Wt
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891.11
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Formula
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C47H58N10O6S
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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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(2S,4R)-4-hydroxy-1-((R)-2-(3-(((S)-1-((R)-3-((S)-2-(2-hydroxyphenyl)-5,6,6a,7,9,10-hexahydro-8H-pyrazino[1',2':4,5]pyrazino[2,3-c]pyridazin-8-yl)pyrrolidin-1-yl)propan-2-yl)oxy)isoxazol-5-yl)-3-methylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
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References
1. Koichi Ito, et al. Mol Cancer Ther (2023) 22 (12_Supplement): B113.
2. Patent WO2024076985 A2.
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