您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > VE-821
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
VE-821
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VE-821图片
CAS NO:1232410-49-9
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
VE-821 是一种有效的 ATP 竞争性的ATR抑制剂,Ki/IC50为 13 nM/26 nM。
生物活性

VE-821 is a potent ATP-competitive inhibitor ofATRwithKi/IC50of 13 nM/26 nM.

IC50& Target

ATR

13 nM (Ki)

ATM

16 μM (Ki)

DNA-PK

2.2 μM (Ki)

PI3Kγ

3.9 μM (Ki)

体外研究
(In Vitro)

VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3Kγ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases[1]. VE-821 (compound 27) also inhibits ATM and DNA-PK wirh IC50of >8 μM, and 4.4 μM, respectively[2]. VE-821 significantly enhances the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and Gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 leads to inhibition of radiation-induced G2/M arrest in cancer cells. In both PSN-1 and MiaPaCa-2 cells, 1 μM VE-821 inhibits phosphorylation of Chk1 (Ser 345) after treatment with Gemcitabine (100 nM), radiation (6 Gy) or both, at 2 h post-irradiation[3].

分子量

368.41

性状

Solid

Formula

C18H16N4O3S

CAS 号

1232410-49-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(135.72 mM;Need ultrasonic)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7144 mL13.5718 mL27.1437 mL
5 mM0.5429 mL2.7144 mL5.4287 mL
10 mM0.2714 mL1.3572 mL2.7144 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:
  • 1.

    VE-821 is prepared im vehicle (10% PEG300, 2.5% Tween-80, pH 4)[4].