| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| D408566-1ml |
1ml |
现货  |
|
| 英文别名 | PS-095760 | (2S)-1-[3-ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Dinaciclib (SCH727965) |
| 生化机理 | Dinaciclib（SCH727965，PS-095760）是一种新型、强效的 CDK 抑制剂，在无细胞实验中对 CDK2、CDK5、CDK1 和 CDK9 的 IC50 分别为 1 nM、1 nM、3 nM 和 4 nM。它还能阻止胸苷（dThd）DNA掺入。Dinaciclib 可通过激活 Caspases 8 和 9 诱导细胞凋亡。第 3 阶段 |
| 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 | 细胞周期蛋白依赖性激酶 9 抑制剂 |
| 产品介绍 |
Dinaciclib (SCH727965)是CDK抑制剂，对CDK2，CDK5，CDK1和CDK9的IC50分别为1 nM，1 nM，3 nM和4 nM。A novel and potent cyclin-dependent kinase inhibitor for Cdk2, Cdk5, Cdk1, and Cdk9 Information Dinaciclib (SCH727965, PS-095760) is a novel and potent CDK inhibitor forCDK2,CDK5,CDK1andCDK9withIC50of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through t Dinaciclib is also a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells with IC50 of 4 nM. Dinaciclib strongly suppresses phosphorylation of Rb on Ser 807/811 at concentrations >6.25 nM, which is in agreement with the observation that 4 nM concentrations are required for 50% inhibition of dThd DNA incorporation in the same cell model. Significantly, complete suppression of Rb phosphorylation is correlated with the onset of apoptosis, as indicated by the appearance of the p85 PARP cleavage product in cells exposed to >6.25 nM Dinaciclib. Dinaciclib is active against a broad spectrum of human tumor cell lines. Addition of Dinaciclib during hydroxyurea exposure also suppresses accumulation of γ-H2AX, in a dose-dependent manner. Dinaciclib inhibits melanoma cell proliferation, and drives melanoma cells into massive apoptosis. Dinaciclib induces the apoptosis of several osteosarcoma cell lines including those resistant to doxorubicin and dasatinib. Dinaciclib attenuates the phosphorylation of RNAP II at serine 2 and the phosphorylation of the CDK inhibitor p27Kip1 at threonine 187. Reductions in phosphorylation activity occurrs at 12 - 40 nM Dinaciclib (4 to 16 hours post-Dinaciclib addition). Dinaciclib also reduces the phosphorylation of Rb at serine 807/811. Dinaciclib induces the apoptosis of mock- and p53-depleted U2OS cells to a similar extent. In vivo Dinaciclib i.p. administration at 8, 16, 32, and 48 mg/kg daily for 10 days results in tumor inhibition by 70%, 70%, 89%, and 96%, respectively. Dinaciclib MED (minimum effective dose) appears to be <8 mg/kg. Dinaciclib is well tolerated, and the maximum body weight loss in the highest dosage group is 5%. Dinaciclib has dose-dependent antitumor activity in vivo, and that nearly complete inhibition of tumor growth occurs at a dose level below the MTD (maximum tolerated dose). Dinaciclib has a short plasma half-life in mouse. cell lines： Concentrations：0 μM -5 μM Incubation Time：24 hours Powder Purity:≥98% |
| ALogP | 1.9 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCC[C@H]4CCO |
| 分子量 | 396.49 |
| Reaxy-Rn | 29384530 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29384530&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 63 mg/mL (200.4 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| 熔点 | 107-111°C |
| 象形图 | GHS08, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H372: 通过长时间或反复暴露对器官造成损害 H340: 可能导致遗传缺陷 |
| 预防措施声明 |
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P281: 根据需要使用个人防护设备。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。 P203: 使用前，获取、阅读并遵守所有安全说明。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P318: 如果暴露或担心，请就医。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。 P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。 P319: 如果你感到不适，请寻求医疗帮助。 |
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