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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) |
|---|
Dinaciclib (SCH727965), 细胞周期蛋白依赖性激酶 9 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
In vitro
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 Data
cell lines：
Concentrations：0 μM -5 μM
Incubation Time：24 hours
Powder Purity:≥98%
规格
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
细胞周期蛋白依赖性激酶 9 抑制剂
名称和识别符
EC号
814-152-8
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=
技术文档
高级数据
产品属性
| ALogP | 1.9 |
|---|
关联靶点（人）
CDK1
Tchem
细胞周期蛋白依赖性激酶 1(Cyclin-dependent kinase 1)
(10 活性数据)
CDK13
Tchem
细胞周期蛋白依赖性激酶 13(Cyclin-dependent kinase 13)
(1 活性数据)
ERCC2
Tchem
通用转录和DNA修复因子IIH解旋酶亚基XPD(General transcription and DNA repair factor IIH helicase subunit XPD)
(1 活性数据)
CHD4
Tchem
色氨酸结构域解旋酶 DNA 结合蛋白 4(Chromodomain-helicase-DNA-binding protein 4)
(1 活性数据)
CDK9
Tchem
细胞周期蛋白依赖性激酶9(Cyclin-dependent kinase 9)
(11 活性数据)
CDK8
Tchem
细胞周期蛋白依赖性激酶 8(Cyclin-dependent kinase 8)
(4 活性数据)
CDK4
Tclin
细胞周期蛋白依赖性激酶4(Cyclin-dependent kinase 4)
(1 活性数据)
CDK2
Tchem
细胞周期蛋白依赖性激酶2(Cyclin-dependent kinase 2)
(12 活性数据)
CDK5
Tchem
细胞周期蛋白依赖性类激酶 5(Cyclin-dependent-like kinase 5)
(10 活性数据)
HSF1
Tchem
热休克因子蛋白1(Heat shock factor protein 1)
(1 活性数据)
AKR1C3
Tchem
醛酮还原酶家族 1 个成员 C3(Aldo-keto reductase family 1 member C3)
(2 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 63 mg/mL (200.4 mM); Water: Insoluble; Ethanol: Insoluble;
熔点
107-111°C
安全和危险性（GHS）
信号词
危险
危险声明
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H340: 可能导致遗传缺陷
H372: 通过长时间或反复暴露对器官造成损害
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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