| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408361-1ml |
1ml |
现货  |
|
| 英文别名 | 2H-Imidazo[4,5-c]quinolin-2-one, 7-fluoro-1,3-dihydro-3-methyl-1-(1-methylethyl)-8-[6-[3-(1-piperidinyl)propoxy]-3-pyridinyl]- |
|---|---|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | ATM 丝氨酸/苏氨酸激酶抑制剂 |
| 产品介绍 |
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. 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 lines： Concentrations：0-1250 nM Incubation Time：1 h Powder Purity:≥99% |
| IC50 | ATM, IC50: 0.78 nM |
|---|---|
| ALogP | 4.231 |
| hba_count | 4 |
| Rotatable Bond | 7 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC(C)N1C(=O)N(C)C2=C1C3=CC(=C(F)C=C3N=C2)C4=CC=C(OCCCN5CCCCC5)N=C4 |
| 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= |
| 溶解性 | Solubility (25°C) In vitro |
|---|---|
| DMSO(mg / mL) Max Solubility | 14 |
| DMSO(mM) Max Solubility | 29.32 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 31033040 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=31033040&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
首页
400-620-6333
