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首页-抗体药物偶连体和PROTACs-PROTAC-PRT3789
PRT3789

Chemical Structure : PRT3789

CAS No.: 2755761-78-3

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PRT3789 (PRT-3789)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 891.11
分子式 C47H58N10O6S
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

(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

参考文献

1. Koichi Ito, et al. Mol Cancer Ther (2023) 22 (12_Supplement): B113.

2. Patent WO2024076985 A2.

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