VE-822

貨號 Cat. No.: S7102
規格 Size: 10mgã€50mg
品牌 Brand: Selleckchem

Description

VE-822

Catalog No.S7102

VE-822 is an ATR inhibitor with IC50 of 19 nM.

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10mg	USD 185	In stock	0 1 2 3 4 5 6 7 8 9 10
50mg	USD 592	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	VE-822 is an ATR inhibitor with IC50 of 19 nM.
Targets	ATR	ATM
IC50	19 nM	34 μM ^[1]
In vitro	VE-822 (80 nM) attenuates ATR signaling pathway and reduces survival in tumor cells in response to XRT and gemcitabine. VE-822 (80 nM) attenuates ATR signaling in normal cells without enhancing radiation and gemcitabine killing in normal cells. VE-822 (80 nM) increases XRT-induced residual γH2AX and 53BP1 foci compared with XRT in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) pre-treatment decreases Rad51 foci after XRT in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) alone increases the G1-phase-fraction in MiaPaCa-2 and PSN-1 cells. VE-822 (80 nM) abrogates XRT enriched G2/M-phase-fraction in MiaPaCa-2 and PSN-1 cells. VE-822 has little effect alone, while VE-822 (80 nM) combined with XRT and/or gemcitabine enhances early and late apoptosis in PSN-1 cells that is strongest in the triple combination. ^[1] VE-822 increases tumor response to DNA damaging agents associated with blockade of pChk1 Ser345. ^[2]
In vivo	VE-822 (60 mg/kg) inhibits phospho-Ser-345-Chk1 in mice bearing PSN-1 tumors after DNA-damaging agents. VE-822 (60 mg/kg) combined with XTR doubles the time for tumors to grow to 600 mm³ of XRT alone in mice bearing both PSN-1 and MiaPaCa-2 tumors. VE-822 (60 mg/kg) added to the combination of gemcitabine and XRT substantially prolongs the tumor growth delay compared with the Gem+XRT1 group n mice bearing both PSN-1 tumors. VE-822 (60 mg/kg) combined with XRT1 increases uptake in tumors by 44% compared with XRT1, suggesting that addition of VE-822 increased γH2AX phosphorylation and persistence of DNA damage caused by XRT. ^[1]
Features	VE-822 is a highly selective and potent derivative of the ATR inhibitor VE-821.

Protocol(Only for Reference)

Animal Study: ^[1]

Animal Models	mice bearing PSN-1 or MiaPaCa-2 tumors
Dosages	60 mg/kg
Administration	Oral gavage

References

Chemical Information

Download VE-822 SDF

Molecular Weight (MW)	463.55
Formula	C₂₄H₂₅N₅O₃S
CAS No.	1232416-25-9

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

Solubility (25°C) *	In vitro	DMSO	36 mg/mL (77 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
* <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.