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KU-0060648

Catalog No. T6557 CAS 881375-00-4

Synonyms: KU0060648

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

KU-0060648, CAS 881375-00-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 196.00
25 mg	In stock	$ 455.00
50 mg	In stock	$ 657.00
100 mg	In stock	$ 918.00

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Purity: 99.21%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.
Targets&IC50	PI3Kα:4 nM, PI3Kβ:0.5 nM, PI3Kδ:0.1 nM
In vitro	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. [1]
In vivo	KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. [1]
Cell Research	SRB assay(Only for Reference)

Synonyms	KU0060648
Molecular Weight	582.71
Formula	C33H34N4O4S
CAS No.	881375-00-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

2eq.HCl: 58.3 mg/mL (100 mM)

References and Literature

1. Munck JM, et al. Mol Cancer Ther, 2012, 11(8), 1789-1798. 2. Celine Cano, et al. Mol Cancer Ther, 2009, 8(12 Suppl), A138.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library PI3K-AKT-mTOR Compound Library Anti-Colorectal Cancer Compound Library Oxidation-Reduction Compound Library Neuronal Differentiation Compound Library Bioactive Compounds Library Max Angiogenesis related Compound Library NO PAINS Compound Library Anti-Prostate Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KU-0060648 881375-00-4 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K mTOR inhibit Phosphoinositide 3-kinase KU0060648 Inhibitor Mammalian target of Rapamycin KU 0060648 DNA-dependent protein kinase inhibitor

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