Description
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.
Product information
CAS Number: 845932-30-1
Molecular Weight: 564.72
Formula: C29H32N4O4S2
Chemical Name: 3-(4-methylpiperazin-1-yl)-N-{6-[6-(morpholin-4-yl)-4-oxo-4H-pyran-2-yl]thianthren-2-yl}propanamide
Smiles: CN1CCN(CCC(=O)NC2=CC3SC4C=CC=C(C=4SC=3C=C2)C2=CC(=O)C=C(O2)N2CCOCC2)CC1
InChiKey: IIBZKDYAYJSSGB-UHFFFAOYSA-N
InChi: InChI=1S/C29H32N4O4S2/c1-31-9-11-32(12-10-31)8-7-27(35)30-20-5-6-24-26(17-20)38-25-4-2-3-22(29(25)39-24)23-18-21(34)19-28(37-23)33-13-15-36-16-14-33/h2-6,17-19H,7-16H2,1H3,(H,30,35)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
In Vivo:
KU59403 with a single daily dose of 12.5 mg/kg causes a significant sensitization. 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.
Products are for research use only. Not for human use.
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