AZ32

ATM 选择性抑制剂 | 活化剂

10mM in DMSO

CAS编号: 2288709-96-4
分子式: C₂₀H₁₆N₄O
分子量: 328.37
PubChem编号: 134814488

有货

库存信息

关闭

货号 (SKU)	包装规格	是否现货	价格	数量
A492017-1ml	1ml	现货

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Compound libraries (12326)

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基本描述

英文别名	N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide
规格或纯度	10mM in DMSO
英文名称	AZ32
生化机理	AZ32 是 ATM 激酶的特异性抑制剂，在小鼠体内具有良好的 BBB 穿透性，对 ATM 酶的 IC50 值小于 0.0062 μM。它对 ATR 具有充分的选择性，同时还具有较高的细胞渗透性。
储存温度	-80℃储存
运输条件	超低温冰袋运输
产品介绍	AZ32是ATM kinase的特异性抑制剂，在小鼠中具有良好的血脑屏障通透性，对ATM酶的IC5值小于0.0062 μM。它具有充分的选择性和高细胞透性。 Information AZ32 is a specific inhibitor of theATM kinasethat possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. Targets ATM (Cell-free assay) <0.0062 μM In vitro AZ32 blocks the DNA damage response (DDR) and radiosensitized GBM cells in vitro. AZ32 shows moderate potency against ATM in cell (IC50 = 0.31 μM) and adequate selectivity over ATR, while also having high cell permeability. In vivo AZ32, with enhanced blood-brain barrier (BBB) penetration, was highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is the first ATMi with oral bioavailability shown to radiosensitize glioma and improve survival in orthotopic mouse models. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free brain concentrations of AZ32 was in excess of the cellular IC50 for approximately 22 hr. AZ32 has enhanced BBB penetration at 8.7-fold and improved brain coverage over AZ31 but with reduced ATM selectivity. Cell Research(from reference) Cell lines：U1242 cells Concentrations：3 μM Incubation Time：48 h

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

IUPAC Name	N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide
INCHI	InChI=1S/C20H16N4O/c1-21-20(25)16-9-7-15(8-10-16)18-11-23-19-12-22-17(13-24(18)19)14-5-3-2-4-6-14/h2-13H,1H3,(H,21,25)
InChi Key	LCRTUEXVVKVKBD-UHFFFAOYSA-N
Canonical SMILES	CNC(=O)C1=CC=C(C=C1)C2=CN=C3N2C=C(N=C3)C4=CC=CC=C4
Isomeric SMILES	CNC(=O)C1=CC=C(C=C1)C2=CN=C3N2C=C(N=C3)C4=CC=CC=C4
PubChem CID	134814488
分子量	328.37

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 66 mg/mL (200.99 mM); Ethanol: 7 mg/mL (21.31 mM); Water: Insoluble;
分子量	328.400 g/mol
XLogP3	3.300
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	3
可旋转键计数Rotatable Bond Count	3
精确质量Exact Mass	328.132 Da
单同位素质量Monoisotopic Mass	328.132 Da
拓扑极表面积Topological Polar Surface Area	59.300 Å²
重原子数Heavy Atom Count	25
形式电荷Formal Charge	0
复杂度Complexity	457.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1