874146-69-7
PK11007
CAS: 874146-69-7
Molecular Formula: C15H11ClFN5O3S2
874146-69-7 - Names and Identifiers
874146-69-7 - Physico-chemical Properties
| Molecular Formula | C15H11ClFN5O3S2 |
| Molar Mass | 427.8609432 |
| Solubility | Soluble in DMSO |
| Storage Condition | 2-8°C |
| Use | PK11000 is an anti-p53 drug. Note: Many vendors mistakenly are selling this drug as PK11007, which CAS# is 874146-69-7 |
874146-69-7 - Reference
| Reference Show more | 1: Duffy MJ, Synnott NC, Crown J. Mutant p53 in breast cancer: potential as atherapeutic target and biomarker. Breast Cancer Res Treat. 2018 Mar 21. doi:10.1007/s10549-018-4753-7. [Epub ahead of print] Review. PubMed PMID: 29564741. 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 targetfor the treatment of triple-negative breast cancer: Preclinical investigationwith 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. PubMed PMID: 29069577. 3: Duffy MJ, Synnott NC, Crown J. Mutant p53 as a target for cancer treatment.Eur J Cancer. 2017 Sep;83:258-265. doi: 10.1016/j.ejca.2017.06.023. Epub 2017 Jul28. Review. PubMed PMID: 28756138. 4: Bauer MR, Joerger AC, Fersht AR. 2-Sulfonylpyrimidines: Mild alkylating agentswith 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.PubMed PMID: 27551077; PubMed Central PMCID: PMC5018792. |
874146-69-7 - Preparation solution concentration reference
| 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 |
| 5 mM | 0.047 ml | 0.234 ml | 0.467 ml |
Last Update：2024-01-02 23:10:35
874146-69-7 - Reference Information
| biological activity | PK11007 is a mild thiol alkylating agent with anticancer activity. PK11007 stabilizes p53 by selective alkylation of both surface-exposed cysteines without affecting its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels. |
| Cell Line: | p53 wild-type cell lines (WI-38, HUH-6, NUGC-4, SJSA-1) and p53 mutant cell lines (HUH-7, NUGC-3, SW480, MKN1) NUGC-4, NUGC-3, MKN1, HUH-6, and HUH-7 cancer cells MKN1, HUH-7, NUGC-3, HUH-6 cells |
| Concentration: | 0 μM, 20 μM, 40 μM, 60 µM, 80 µM, 100 µM and 120 µM 0 μM, 15 μM, 30 μM, 60 µM 15 μM, 20 μM |
| Incubation Time: | 24 hours 3 hours or 6 hours 4.5 hours or 6 hours |
| Result: | There was a large viability reduction in mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S) and in p53 WT cell line SJSA-1 at concentrations ranging from 15 to 30 µM. The p53 WT cancer cell lines HUH-6, NUGC-4 and WI-38 were less sensitive with reduced cell viability only at high concentrations of compound (60 and 120 µM). Up-regulated 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. Also increased p53 activity in HUH-6 and NUGC-4 cells, as indicated by the increase of MDM2, PUMA, and p21 protein levels. Increased transcription of p53 target genes in three mutant p53 cell lines after 6-h treatment. PUMA and p21 mRNA levels were 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 were halved in MKN1 and NUGC-3 cells. |
Last Update：2024-04-09 15:16:57
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Product Name: PK11007 Visit Supplier Webpage Request for quotationCAS: 874146-69-7
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Mobile: 18021002903
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Wechat: 18301782025
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