PK11007

98.70%

PK11007

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品牌：源叶(MedMol)

产品编号：S89197 一键复制产品信息

CAS号：874146-69-7

分子式：C₁₅H₁₁ClFN₅O₃S₂

分子量：427.86

别名：PK11000; PK 11000; PK-11000; PK11007-analog; PK-11007-analog; PK 11007-analog;

货号	规格	价格	上海	北京	珠海	重庆	武汉
S89197-2mg促销	98.70%	￥160.00 ￥128.00 S89197-2mg ￥128.00 现货	9 9	-	-	-	-
S89197-5mg促销	98.70%	￥260.00 ￥208.00 S89197-5mg ￥208.00 现货	5 5	-	-	-	-
S89197-25mg促销	98.70%	￥870.00 ￥696.00 S89197-25mg ￥696.00 现货	3 3	-	-	-	-

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产品介绍参考文献(1篇) 质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels

靶点：

MDM-2/p53; Reactive Oxygen Species;ReactiveOxygenSpecies; p53

体外研究：

PK11007 (0-120 µM; 24 hours; four p53 wild-type cell lines and fours p53 mutant cell lines) treatment results in a large viability reduction in mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S) at concentrations ranging from 15 to 30 µM. PK11007 induces mainly caspase-independent cell death. PK11007 (0-60 µM; 3 hours or 6 hours; NUGC-4, NUGC-3, MKN1, HUH-6, and HUH-7 cancer cells) treatment up-regulates 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, suggesting partial restoration of transcriptional activity to destabilized p53 mutants. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells, as indicated by the increase of MDM2, PUMA, and p21 protein levels. PK11007 (15-20 µM; 4.5 hours or 6 hours; MKN1, HUH-7, NUGC-3, HUH-6 cells) treatment increases transcription of p53 target genes in three mutant p53 cell lines after 6-h treatment. PUMA and p21 mRNA levels are up-regulated by a factor of 2 upon treatment of NUGC-3, MKN, and HUH-7 cells, as well as NOXA for the latter two. MDM2 levels are halved in MKN1 and NUGC-3 cells. PK11007 viability reduction is potentiated by glutathione depletion. To test whether PK11007 also increases ROS levels, NUGC-3, NUGC-4, HUH-6, HUH-7, and MKN1 cells with PK11007 are incubated for 2 h. There are elevated ROS levels in all cell lines after 2 h. In the mutant p53 cells MKN1, HUH-7, and NUGC-3, h

参考文献：

1. Bauer MR, et al. 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. 2. Synnott NC, et al. 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

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.337 ml	11.686 ml	23.372 ml
5 mM	0.467 ml	2.337 ml	4.674 ml
10 mM	0.234 ml	1.169 ml	2.337 ml
50 mM	0.047 ml	0.234 ml	0.467 ml