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AZ32 是一种口服生物利用度和血脑屏障穿透性 ATM 抑制剂,对 ATM 酶的 IC50 <6.2 nM,对细胞内 ATM 的 IC50 为 0.31 μM。
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AZ32 是一种口服生物利用度和血脑屏障穿透性 ATM 抑制剂,对 ATM 酶的 IC50 <6.2 nM,对细胞内 ATM 的 IC50 为 0.31 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 365 | 现货 | |
2 mg | ¥ 523 | 现货 | |
5 mg | ¥ 828 | 现货 | |
10 mg | ¥ 1,320 | 现货 | |
25 mg | ¥ 2,320 | 现货 | |
50 mg | ¥ 3,530 | 现货 | |
100 mg | ¥ 4,970 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 892 | 现货 |
产品描述 | AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for ATM enzyme, and an IC50 of 0.31 μM for ATM in cell. |
靶点活性 | ATM:0.31 μM (in cell), ATM:6.2 nM |
体外活性 | AZ32 is an enhanced blood-brain barrier (BBB)-penetrating ATM inhibitor. AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro[1]. |
体内活性 | AZ32 has enhanced BBB penetration that is highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC50 for approximately 22 hours[1]. |
分子量 | 328.37 |
分子式 | C20H16N4O |
CAS No. | 2288709-96-4 |
Smiles | CNC(=O)c1ccc(cc1)-c1cnc2cnc(cn12)-c1ccccc1 |
密度 | 1.25 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (167.49 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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