|5-氯-2-(甲基磺酰基)嘧啶-4-羧酸|CsnPharm

CAS No.: 38275-34-2

5-Chloro-2-(methylsulfonyl)pyrimidine-4-carboxylic acid Catalog No. CSN22900

Synonyms: PK-11000

PK11007 is a p53 targeting compond anti-tumor activities.

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生物活性

描述The tumor suppressor p53 plays a key role in regulating cell cycle arrest, DNA repair, apoptosis, and cell senescence and is inactivated either by mutation or up-regulation of proteins such as MDM2 or MDMX in virtually all human cancers. Cancers with mutant p53 often show increased metastasis, genomic instability, and higher chemoresistance. PK11007, a thiol-modifying compound, exerts antitumor function via reactivating p53. PK11007 increased protein levels of the p53 target genes p21, MDM2, and PUMA in a mostly concentration-dependent manner in NUGC-3 (p53-Y220C), HUH-7 (p53-Y220C) and MKN1 (p53-V143A) cells and also activated the unfolded protein response pathway in a concentration-dependent manner in HUH-7 cells. PK11007 slightly increased caspase 3/7 activity without inducing membrane permeabilization in SW480 (15% increase at 15 μM), SJSA-1 (40% increase at 30 μM), and HCT116 (10% increase at 60 μM) cells, and depleted GSH and increased concentration of ROS^[1]. PK11007 was found to induce apoptosis in both a time and concentration-dependent manner in the two p53-mutated triple-negative breast cancer cell lines investigated, HCC1143 and MDA-MB-468, but not in the WT-p53 cell line, MCF-7^[2].
作用机制PK11007 stabilizes p53 in vitro via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity.
参考文献

[1] Bauer MR, Joerger AC, Fersht AR. 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5271-80. doi: 10.1073/pnas.1610421113. Epub 2016 Aug 22. PMID: 27551077; PMCID: PMC5018792.
[2] Synnott NC, Bauer MR, Madden S, Murray A, Klinger R, O'Donovan N, O'Connor D, Gallagher WM, Crown J, Fersht AR, Duffy MJ. Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007. Cancer Lett. 2018 Feb 1;414:99-106. doi: 10.1016/j.canlet.2017.09.053. Epub 2017 Oct 22. PMID: 29069577.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.2260 mL
- 21.1298 mL
- 42.2596 mL
- 5 mM
- 0.8452 mL
- 4.2260 mL
- 8.4519 mL
- 10 mM
- 0.4226 mL
- 2.1130 mL
- 4.2260 mL

技术信息

CAS号

38275-34-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C6H5ClN2O4S

运输

蓝冰

分子量

236.63

别名

PK-11000

溶解度

DMSO	270.0 mg/mL (1141.0 mM)
Water	150.0 mg/mL (633.9 mM) warming

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5-Chloro-2-(methylsulfonyl)pyrimidine-4-carboxylic acid Catalog No. CSN22900

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