KU 59403
CAS No. : 845932-30-1
| Size | Price | Stock |
|---|---|---|
| 5mg | $350 | In-stock |
| 10mg | $550 | In-stock |
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| 100 mg | Get quote | |
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| Cat. No. : | HY-18650 |
| M.Wt: | 564.72 |
| Formula: | C29H32N4O4S2 |
| Purity: | >98 % |
| Solubility: | DMSO : 10 mg/mL (ultrasonic;warming;heat to 60°C) |
KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively[1].
IC50 & Target: IC50: 3 nM (ATM)[1].
In Vitro: KU 59403 (1 μM) enhances 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. 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[1].
In Vivo: KU59403 with a single daily dose of 12.5 mg/kg causes a significant sensitization[1].
Increasing the dose of KU59403 to 25 mg/kg given twice daily results in the greatest chemo-sensitisation with a 3-fold increase in BMY-40481-induced tumour growth delay in both SW620 and HCT116-N7 xenografts, in the absence of a significantly increased toxicity[1].
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