2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR
  4. KU 59403

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.

For research use only. We do not sell to patients.

KU 59403 Chemical Structure

KU 59403 Chemical Structure

CAS No. : 845932-30-1

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Based on 1 publication(s) in Google Scholar

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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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KU 59403 Related Antibodies

Cell Viability Assay[1]

Cell Line: LoVo, HCT116 and SW620 (human colon cancer), and U2OS (human osteosarcoma) and MDA-MB-231 (human breast cancer) cells.
Concentration: 1 μM.
Incubation Time: 16 hours.
Result: Had at least 1000 times greater specificity for ATM over other members of the PI3K family tested.
Enhanced camptothecin cytotoxicity in both cell lines with greater enhancement being observed in the LoVo compared to the SW620 cells.
Significantly enhanced the cytotoxicity of fixed concentrations of VP-16 (0.1 and 1 μM) or NSC 123127 (10 or 100 nM) in these cell lines, with greater enhancement of VP-16 in SW620 cells and of NSC 123127 in LoVo cells.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 nude mice implanted with SW620 or HCT116-N7 human cancer cell lines at 1×107 cells per animal s.c. (n=5 per group)[1].
Dosage: 6, 12.5 and 25 mg/kg.
Administration: I.P. twice daily (0 and 4 hours) and 12.5 mg/kg once daily.
Result: Treatment with BMY-40481 alone causes a modest tumour growth delay of 4 days (time to RTV4=10.5 days). This delay is extended to 8.5 days when given with KU 59403 at 12.5 mg/kg i.p. twice daily for 5 days and 11.5 days (time to RTV4=18 days) when given with KU 59403 at 25 mg/kg i.p. twice daily for 5 days.
Molecular Weight

564.72

Formula

C29H32N4O4S2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(NC(C=C1S2)=CC=C1SC3=C2C=CC=C3C4=CC(C=C(N5CCOCC5)O4)=O)CCN6CCN(C)CC6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (17.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7708 mL 8.8539 mL 17.7079 mL
5 mM 0.3542 mL 1.7708 mL 3.5416 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.23%

COA (247 KB) HNMR (152 KB) RP-HPLC (120 KB) MS (103 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7708 mL 8.8539 mL 17.7079 mL 44.2697 mL
5 mM 0.3542 mL 1.7708 mL 3.5416 mL 8.8539 mL
10 mM 0.1771 mL 0.8854 mL 1.7708 mL 4.4270 mL
15 mM 0.1181 mL 0.5903 mL 1.1805 mL 2.9513 mL
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KU 59403 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KU 59403845932-30-1KU59403KU-59403ATM/ATRAtaxia telangiectasia mutatedATM and RAD3 relatedInhibitorinhibitorinhibit

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