KU 59403 is an effective ATM inhibitor (IC50: 3 nM, 9.1 μM, and 10 μM for ATM, DNA-PK, and PI3K, respectively).

Inhibition of IR-induced ATM activity by KU 59403 (1 μM) is approximately 50% in MDA-MB231 cells and >50% in HCT116 cells that have low ATM expression and activity. KU 59403 (1 μM) increases VP-16 (1 μM) cytotoxicity to a similar extent in HCT116 and HCT116-N7 cells, and in the p53 mutant SW620 cells and human breast cancer cell line, MDAMB-231, sensitisation is 11.9±4.7 and 3.8±1.8-fold respectively [1].

KU59403 with a single daily dose of 12.5 mg/kg induces an obvious sensitization. Increasing the dose of KU59403 to 25 mg/kg given twice daily causes the greatest chemo-sensitisation. In the absence of a significantly increased toxicity, It has a 3-fold increase in BMY-40481-induced tumour growth delay in both SW620 and HCT116-N7 xenografts [1].

845932-30-1

C29H32N4O4S2

564.72

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years