| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| K408825-1ml |
1ml |
现货  |
|
| 英文别名 | 2-((2S,6R)-2,6-dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl)acetamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | KU-60019 |
| 生化机理 | KU-60019 是 KU-55933 的改进类似物，在无细胞实验中对 ATM 的 IC50 值为 6.3 nM，对 ATM 的选择性分别是 DNA-PK 和 ATR 的 270 倍和 1600 倍，是一种高效的放射增敏剂。 |
| 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 |
KU-60019是KU-55933的改良类似物，对ATM的IC50为6.3 nM。 Information KU-60019 is an improved analogue of KU-55933, withIC50of 6.3 nM forATMin cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. Compared to KU-55933, KU-60019 is an improved inhibitor of the ATM kinase, while displaying similar target selectivity. KU-60019 has little activity against DNA-PKcs and ATR with IC50 values of 1.7 μM and >10 μM, respectively, as well as 229 other protein kinases such as PI3K, mTOR and mTOR/FKBP12. KU-60019 displays 3- to 10-fold more potency than KU-55933 at blocking radiation-induced phosphorylation of key ATM protein targets such as p53, γ-H2AX, and CHK2, in human glioma U87 and U1242 cells, as 1 μM of KU-60019 significantly induces >70% decrease of p53 (S15) phosphorylation to which extent ~10 μM of KU-55933 is required to achieve. KU-60019 effectively radiosensitizes human glioma cells with dose-enhancement ratio of 1.7 and 4.4 at 1 μM and 10 μM, respectively, and also radiosensitizes the normal fibroblasts but not the A-T fibroblasts. KU-60019 treatment (3 μM) blocks basal and insulin-induced AKT S473 phosphorylation by 70% and ~50%, respectively, and completely reduces radiation-induced AKT phosphorylation below the level of control. The effect of KU-60019 on AKT S473 phosphorylation can be seen in glioma cell lines and normal fibroblasts but not in A-T (h-TERT) cells, and can be significantly blocked by phosphatase inhibitor okadaic acid, suggesting a critical role of ATM kinase in regulating AKT phosphorylation via unknown phosphatase. Consistent with the inhibition of prosurvival AKT signaling, KU-60019 at 3 μM significantly inhibits migration and invasion of human glioma U87 cells by >70% and ~60%, respectively, as well as U1242 cells by >50% and ~60% respectively. In vivo In orthotopic glioma U1242/luc-GFP xenograft models, the combination of KU-60019 and radiation significantly increases survival of mice than KU-60019 alone, radiation alone, or no treatment. In addition, p53-mutant gliomas is much more sensitive to KU-60019 radiosensitization than wild-type glioma. cell lines： Concentrations：Dissolved in water, final concentrations ~3 μM Incubation Time：1, 3, and 5 days Powder Purity:≥97% |
| IC50 | ATM, IC50: 6.3 nM |
|---|---|
| ALogP | 3.818 |
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC1CN(CC(C)O1)CC(=O)NC2=CC3=C(SC4=C(C3)C=CC=C4C5=CC(=O)C=C(O5)N6CCOCC6)C=C2 |
| 分子量 | 547.67 |
| Reaxy-Rn | 15466363 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15466363&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 55 mg/mL (197.06 mM); Water: 55 mg/mL (197.06 mM); Ethanol: 55 mg/mL (197.06 mM); |
|---|---|
| DMSO(mg / mL) Max Solubility | 18 |
| DMSO(mM) Max Solubility | 32.87 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 15466363 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15466363&ln= |
| Concentration(Compounding value) | 9-11（mmol/L） |
|---|---|
| Record the entire process by video | Conform |
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