| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A422681-1ml |
1ml |
现货  |
|
| 英文别名 | 7-methyl-2-[(7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(oxan-4-yl)purin-8-one | SB23233 | A930641 | BCP30676 | AC-31586 | 7,9-Dihydro-7-methyl-2-[(7-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(tetrahydro-2H-pyran-4-yl)-8H-purin-8-one | S |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | AZD7648 |
| 生化机理 | AZD7648 是一种强效的 DNA-PK 抑制剂，生化试验的 IC50 值为 0.6 nM，对其他 396 种激酶的选择性超过 100 倍。 |
| 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 | 抑制磷脂酰肌醇-4;5-二磷酸 3-激酶催化亚基 alpha；抑制磷脂酰肌醇-4;5-二磷酸 3-激酶催化亚基 gamma；抑制蛋白激酶；DNA 激活；催化亚基 |
| 产品介绍 |
AZD7648是DNA-PK的有效抑制剂，IC50为0.6 nM，其选择性比对所检测激酶库中其他的396种激酶高100倍以上。 AZD-7648 诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。 Information AZD7648 AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases. Targets DNA-PK (Cell-free assay) 0.6 nM In vitro AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, AZD7648 (≥1 µM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone. In vivo AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with olaparib or radiation. |
| ALogP | 1.059 |
|---|---|
| hba_count | 6 |
| HBD Count | 1 |
| Rotatable Bond | 3 |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 未知 |
|---|---|
| IUPAC Name | 7-methyl-2-[(7-methyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)amino]-9-(oxan-4-yl)purin-8-one |
| INCHI | InChI=1S/C18H20N8O2/c1-11-7-15-20-10-21-25(15)9-13(11)22-17-19-8-14-16(23-17)26(18(27)24(14)2)12-3-5-28-6-4-12/h7-10,12H,3-6H2,1-2H3,(H,19,22,23) |
| InChi Key | XISVSTPEXYIKJL-UHFFFAOYSA-N |
| Canonical SMILES | CC1=CC2=NC=NN2C=C1NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCOCC5 |
| Isomeric SMILES | CC1=CC2=NC=NN2C=C1NC3=NC=C4C(=N3)N(C(=O)N4C)C5CCOCC5 |
| 分子量 | 380.4 |
| Reaxy-Rn | 33031239 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=33031239&ln= |
| DMSO(mg / mL) Max Solubility | 6 |
|---|---|
| DMSO(mM) Max Solubility | 15.7728706624606 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 380.400 g/mol |
| XLogP3 | 1.000 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 3 |
| 精确质量Exact Mass | 380.171 Da |
| 单同位素质量Monoisotopic Mass | 380.171 Da |
| 拓扑极表面积Topological Polar Surface Area | 101.000 Ų |
| 重原子数Heavy Atom Count | 28 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 588.000 |
| 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 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Appearance(Colorless to light yellow liquid) | Pass |
| Record the entire process by video | Conform |
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