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KU 59403

CAS No. : 845932-30-1

MCE 国际站：KU 59403

产品活性：KU 59403 是 ATM 的一个有效抑制剂，其对 ATM、DNA-PK 和 PI3K 的 IC₅₀ 值分别为 3 nM、9.1 μM 和 10 μM。

研究领域：Cell Cycle/DNA Damage  |  PI3K/Akt/mTOR

作用靶点：ATM/ATR

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.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Anti-Obesity Compound Library  |  Glucose Metabolism Compound Library  |  Cancer Stem Cells Compound Library  |  Tuvusertib  |  Elimusertib  |  CGK733  |  AZD1390  |  Ceralasertib  |  AZD-7648  |  VE-821  |  KU-55933  |  ATM Inhibitor-3  |  Elimusertib-d₃  |  ATR-IN-22  |  ATR-IN-6  |  AZD0156  |  CP-466722  |  Antitumor agent-28  |  ATR-IN-12  |  ATR-IN-18  |  ATR-IN-13  |  ATR-IN-5  |  ATR-IN-20  |  ATR-IN-21  |  AZ32  |  ATM Inhibitor-2  |  ATM Inhibitor-6  |  Ro 90-7501  |  ATR-IN-17  |  A011  |  ATR-IN-4

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