AZ31

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AZ31

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:

2088113-98-6

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

AZ31 是有效的、高选择性、具有口服活性的ATM的抑制剂，对 ATM 酶的IC₅₀值<1.2 nM，对细胞内 ATM 的IC₅₀值为 46 nM。AZ31 表现出优异的 ATR 选择性 (>500 倍) 、PIKK 家族选择性和泛激酶选择性。AZ31 是一种强效的体外放射增敏剂，可用于癌症的研究。

生物活性

AZ31 is a a potent, highly selective, and orally activeATMinhibitor with anIC₅₀of<1.2 nM forATMenzyme, and anIC₅₀of 46 nM forATMin cell. AZ31 shows excellent selectivity overATR(>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research ofcancer^[1].

IC₅₀& Target^[1]

ATM

1.2 nM (IC₅₀)

ATM

46 nM (IC₅₀, in cell)

体外研究
(In Vitro)

AZ31 (0.3-3 μM; 1 h) affects phosphorylation of a panel of ATM targets^[1].
AZ31 (10 μM; 1 h) affects stabilization of p53 in H2228 lung cancer cells after radiation^[1].

Western Blot Analysis^[1]

Cell Line:	Human glioma cell line
Concentration:	0.3, 1 and 3 μM
Incubation Time:	1 hour
Result:	Blocked phosphorylation of p53-S15, KAP1-S824, and ATM auto-phosphorylation at S1981.

Western Blot Analysis^[1]

Cell Line:	H460 and mutant p53 H2228 cell lines
Concentration:	10 μM
Incubation Time:	1 hour
Result:	Destabilized p53 of mutant p53 but not wild-type after radiation.

体内研究
(In Vivo)

AZ31 (50-100 mg/kg; p.o. twice a day) shows low brain coverage^[1].

Animal Model:	Nude mice^[1]
Dosage:	50 and 100 mg/kg
Administration:	Oral gavage; 50 and 100 mg/kg twice a day
Result:	Exhibited exposure over IC₅₀at 0.046 μM in brain only for 2-3 hours.

分子量

420.50

Formula

C₂₄H₂₈N₄O₃

CAS 号

2088113-98-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.