874146-69-7
Chemical Structure
PK11007
- CAS No.: 874146-69-7
- Formula:C15H11ClFN5O3S2
- Molecular Weight:427.86
IUPAC Name: 5-chloro-2-((4-fluorobenzyl)sulfonyl)-N-(5-methyl-1,3,4-thiadiazol-2-yl)pyrimidine-4-carboxamide
InChIKey: IVZQUWCWXYFPOQ-UHFFFAOYSA-N
SMILES: O=C(C1=NC(S(=O)(CC2=CC=C(F)C=C2)=O)=NC=C1Cl)NC3=NN=C(C)S3
Biological Activity: 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[1][2].
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PK11007 | 98.73% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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 [Content Brief]
Keywords