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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
AZD1390, ATM 丝氨酸/苏氨酸激酶抑制剂
有货
概述
AZD1390是一种具有口服活性的、能穿透中枢神经系统的ATM抑制剂，在细胞中IC50为0.78 nM。它对ATM的选择性是对PIKK家族其他相关酶的10,000以上，具有良好的选择性。
Information
AZD1390 is a first-in-class orally available and CNS penetrantATMinhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.
In vitro
AZD1390 blocks ATM-dependent DDR (DNA damage response) pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 results in increased genome instability.
In vivo
AZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog). It can efficiently cross the BBB in non-human primate PET studies. Profound tumor regressions and increased animal survival (>50 days) have been observed in orthotopic xenograft models of brain cancer following just 2 or 4 days combination treatment of AZD1390 with radiotherapy, compared to radiotherapy treatment alone. In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, AZD1390 dosed in combination with daily fractions of IR (whole-brain or stereotactic radiotherapy) significantly induces tumor regressions and increased animal survival compared to IR treatment alone. AZD1390 has favorable physical, chemical, PK, and PD properties suitable for clinical applications that require exposures within the central nervous system.
Cell Data
cell lines：
Concentrations：0-1250 nM
Incubation Time：1 h
Powder Purity:≥99%
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AZD1390
生化机理
AZD1390 是第一类可口服的中枢神经系统穿透性 ATM 抑制剂，在细胞中的 IC50 值为 0.78 nM，对与之密切相关的 PIKK 酶家族成员的选择性大于 10,000 倍，对多种激酶具有出色的选择性。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
ATM 丝氨酸/苏氨酸激酶抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)N1C2=C(C=NC3=CC(=C(C=C32)C4=CN=C(C=C4)OCCCN5CCCCC5)F)N(C1=O)C
分子量
477.57
Reaxy-Rn
31033040
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31033040&ln=
高级数据
产品属性
| IC50 | ATM, IC50: 0.78 nM |
|---|---|
| ALogP | 4.231 |
| hba_count | 4 |
| Rotatable Bond | 7 |
关联靶点（人）
ATM
Tchem
丝氨酸蛋白激酶 ATM(Serine-protein kinase ATM)
(1 活性数据)
KCNH2
Tclin
钾电压门控通道亚家族 H 成员 2(Potassium voltage-gated channel subfamily H member 2)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro
DMSO(mg / mL) Max Solubility
14
DMSO(mM) Max Solubility
29.3150742299558
Water(mg / mL) Max Solubility
＜1
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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