bs-83759C

DATASHEET

Formulation White solid

Storage: -20°C

Product Information:

PK11007 reactivates mutant p53 via selective alkylation of two cysteine residues without compromising DNA-binding ability.1 p53 target genes p21 and PUMA were activated by treatment with PK11007. Mutant p53-containing cancer cells were more sensitive to PK11007 than wild-type with mutant cells showing greatly reduced viability. It also generated high levels of reactive oxygen species and induced ER stress in a p53-independent (and dependent on glutathione depletion) manner that resulted in cell death. PK11007 inhibited cellular proliferation, induced apoptosis, and blocked cell migration in a panel of 17 breast cancer lines including triple-negative breast cancer (IC50s: 2.3 to 42.2 µM).2

Description:

CAS Number: 874146-69-7 Chemical Name: 5-Chloro-2-[(4-fluorophenyl)methylsulfonyl]-N-(5-methyl-1,3,4-thiadiazol-2-yl)pyrimidine-4-carboxamide Molecular Weight: 427.85 Formula: C15H11ClFN5O3S2 Solubility: DMSO (>25 mg/ml) Physical Properties: White solid Purity: >98% by HPLC NMR (Conforms)