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首页-小分子抑制剂&激动剂-Apoptosis-MDM2-p53-PC14586
PC14586

Chemical Structure : PC14586

CAS No.: 2636846-41-6

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PC14586 (Rezatapopt, PC-14586)

货号: PC-23083Not For Human Use, Lab Use Only.

Rezatapopt (PC14586) is a first-in-class, orally bioavailable Y220C mutant p53 reactivator, binds to the pocket created by the TP53 Y220C mutation (KD=2.5 nM), restoring p53 function.

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5 mg ￥980 In stock
10 mg ￥1580 In stock
25 mg ￥2780 In stock
50 mg ￥4580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Rezatapopt (PC14586) is a first-in-class, orally bioavailable Y220C mutant p53 reactivator, binds to the pocket created by the TP53 Y220C mutation (KD=2.5 nM), restoring p53 function.
PC14586 stabilizes the Y220C mutant in the wild type conformation, resulting in reactivation of p53 transcriptional activity and subsequent expression of its target proteins (e.g. p21, MDM2, Bax, PUMA) in Y220C mutant human cell lines.
PC14586 is highly selective to Y220C mutant cells and results in arrest of the cell cycle in vitro (IC50 ~0.230-1.8 μM).
Oral administration of PC14586 results in a dose responsive anti-tumor effect, with a target efficacious dose of 100 mg/kg daily resulting in approximately 80% tumor regression after 3 weeks in nude mice bearing Y220C mutant NUGC3 gastric cancer xenograft tumors.
PC14586 was shown to convert Y220C mutant to the wildtype conformation, resulting in activation of p53 transcription.

物理化学性质&存储条件

分子量 545.58
分子式 C28H31F4N5O2
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

4-((3-(4-(((3S,4R)-3-fluoro-1-methylpiperidin-4-yl)amino)-1-(2,2,2-trifluoroethyl)-1H-indol-2-yl)prop-2-yn-1-yl)amino)-3-methoxy-N-methylbenzamide

参考文献

1. Melissa Dumble, et al. Cancer Res (2021) 81 (13_Supplement): LB006.

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