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Purity: ≥98%
KU0060648 HCl is a novel, potent and dual inhibitor of DNA-dependent protein kinase (DNA-PK) and PI3Kα/β/δ (Phosphoinositide 3-kinases) with potential antitumor activity. It inhibits DNA-PK and PI3Kα/β/δ with an IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively. It exhibits 20-1000 fold higher selectivity for DNA-PK over other PIKKs and a panel of 60 other kinases.
| ln Vitro |
In vitro activity : KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only by 55% in SW620 cells. In clonogenic survival assays, KU-0060648 increases the cytotoxicity of etoposide and doxorubicin across the panel of DNA-PKcs-proficient cells, but not in DNA-PKcs-deficient cells, confirming that enhanced cytotoxicity of the topoisomerase II poisons etoposide and doxorubicin is due to DNA-PK inhibition.
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| ln Vivo |
In mice bearing SW620 and MCF7 xenografts, KU-0060648 concentrations that were sufficient for in vitro growth inhibition and chemosensitization were maintained within the tumor at nontoxic doses for at least 4 hours. KU-0060648 alone delayed the MCF7 xenografts growth and increased etoposide-induced tumor growth delay in both in MCF7 and SW620 xenografts by up to 4.5 folds, without causing etoposide toxicity to unacceptable levels
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| Animal Protocol |
Mice bearing SW620 and MCF7 xenografts
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| References |
Mol Cancer Ther.2012 Aug;11(8):1789-98.
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| Molecular Formula |
C₂₇H₂₉CL₂N₇O₂S
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|---|---|
| Molecular Weight |
586.54
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| Related CAS # |
881375-00-4
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
O=C(NCC1=CC=C(S(C2=CC(F)=CC(F)=C2)(=O)=O)C=C1)C3=CN4C(C=C3)=NC=C4.Cl
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| Synonyms |
KU-0060648 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~10 mM
Water: N/A Ethanol: N/A |
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| Solubility (In Vivo) |
30% propylene glycol, 5% Tween 80, 65% D5W: 20mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7049 mL | 8.5246 mL | 17.0491 mL | |
| 5 mM | 0.3410 mL | 1.7049 mL | 3.4098 mL | |
| 10 mM | 0.1705 mL | 0.8525 mL | 1.7049 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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