KU-0060648

貨號 Cat. No.: S8045
規格 Size: 2mgã€25mg
品牌 Brand: Selleckchem

Description

KU-0060648

Catalog No.S8045

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.

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2mg	USD 185	In stock	0 1 2 3 4 5 6 7 8 9 10
25mg	USD 1096	In stock	0 1 2 3 4 5 6 7 8 9 10

Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Biological Activity

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	DNA-PK	PI3Kα	PI3Kβ	PI3Kδ
IC50	8.6 nM ^[2]	4 nM	0.5 nM	0.1 nM^[1]
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]
Features

Protocol(Only for Reference)

Cell Assay: ^[1]

Cell lines	MCF7, T47D, MDA-MB-231, LoVo and SW620
Concentrations	~1 μM
Incubation Time	5 day
Method	SRB assay

Animal Study: ^[1]

Animal Models	human-tumor SW620 or MCF7 xenograft models
Dosages	10 mg/kg, twice daily
Administration	i.p.
Solubility	30% propylene glycol, 5% Tween 80, 65% D5W, 20 mg/mL

References

Chemical Information

Download KU-0060648 SDF

Molecular Weight (MW)	582.71
Formula	C₃₃H₃₄N₄O₄S
CAS No.	881375-00-4

Storage	3 years -20â„ƒPowder
Storage	6 months-80â„ƒin DMSO
Syonnyms	N/A

Solubility (25°C) *	In vitro	DMSO	0.4 mg/mL (<1 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W,	20 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.