VE-821

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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。

CAS NO:

1232410-49-9

VE-821 是一种有效的 ATP 竞争性的ATR抑制剂，K_i/IC₅₀为 13 nM/26 nM。

生物活性

VE-821 is a potent ATP-competitive inhibitor ofATRwithK_i/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 (K_is 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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	2.7144 mL	13.5718 mL	27.1437 mL
5 mM	0.5429 mL	2.7144 mL	5.4287 mL
10 mM	0.2714 mL	1.3572 mL	2.7144 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].