WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 408058
Description: PK11007 is an anti-p53 drug. PK11007 preferentially decreases viability in p53-compromised cancer cell lines IC50 values for inhibition of proliferation in a panel of 17 breast cell lines by PK11007 ranged from 2.3 to 42.2 μM. PK11007 induced apoptosis in p53 mutant cell lines. PK11007 is a potential approach for treating p53-mutated breast cancer, including the subgroup with TN disease. Note: Many vendors are selling PK11007 with wrong structure (the product they are selling is actually PK11000).
MedKoo Cat#: 408058
Chemical Formula: C15H11ClFN5O3S2
Exact Mass: 426.9976
Molecular Weight: 427.8534
Elemental Analysis: C, 42.11; H, 2.59; Cl, 8.29; F, 4.44; N, 16.37; O, 11.22; S, 14.99
Synonym: PK11007; PK-11007; PK 11007;
IUPAC/Chemical Name: 5-chloro-2-((4-fluorobenzyl)sulfonyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)pyrimidine-4-carboxamide
InChi Key: IVZQUWCWXYFPOQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H11ClFN5O3S2/c1-8-21-22-14(26-8)20-13(23)12-11(16)6-18-15(19-12)27(24,25)7-9-2-4-10(17)5-3-9/h2-6H,7H2,1H3,(H,20,22,23)
SMILES Code: O=C(C1=NC(S(=O)(CC2=CC=C(F)C=C2)=O)=NC=C1Cl)NC3=NN=C(C)S3
The identification of a targeted therapy for patients with triple-negative breast cancer (TNBC) is one of the most urgent needs in breast cancer therapeutics. The p53 gene is mutated in approximately 80% of patients with TNBC, and is a potential therapeutic target for patients with this form of breast cancer
1: Duffy MJ, Synnott NC, Crown J. Mutant p53 in breast cancer: potential as a therapeutic target and biomarker. Breast Cancer Res Treat. 2018 Jul;170(2):213-219. doi: 10.1007/s10549-018-4753-7. Epub 2018 Mar 21. 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 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. 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 Jul 28. Review. PubMed PMID: 28756138.
4: 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. PubMed PMID: 27551077; PubMed Central PMCID: PMC5018792.