BMS-265246
BMS-265246是一种有效的选择性CDK1/2抑制剂，无细胞试验中IC50为6 nM/9 nM。作用于CDK1/2 比作用于CDK4选择性高25倍。
BMS-265246 Chemical Structure
CAS: 582315-72-8
产品质控
批次：
纯度：
99.79%
99.79
BMS-265246相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HCT116 | Function assay | 1 to 5 uM | 24 hrs | Inhibition of CDK5/p25 in human HCT116 cells assessed as induction of dephosphorylation of FAK at Ser732 residue at 1 to 5 uM after 24 hrs by Western blot analysis | 30234987 |
| HCT116 | Cell cycle assay | 24 hrs | Induction of cell cycle arrest in CDK2 knocked out human HCT116 cells assessed as accumulation at G2/M phase at 0.8 to 5.9 after 24 hrs by propidium iodide-staining based flow cytometry | 30234987 | |
| Sf9 | Function assay | Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay, IC50=0.006μM | 30234987 | ||
| Sf9 | Function assay | Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay, IC50=0.014μM | 30234987 | ||
| Sf9 | Function assay | Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay, IC50=0.222μM | 30234987 | ||
| Sf9 | Function assay | Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay, IC50=0.258μM | 30234987 | ||
| Sf9 | Function assay | Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay, IC50=1.6μM | 30234987 | ||
| Sf9 | Function assay | Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay, IC50=1.8μM | 30234987 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | BMS-265246是一种有效的选择性CDK1/2抑制剂，无细胞试验中IC50为6 nM/9 nM。作用于CDK1/2 比作用于CDK4选择性高25倍。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | BMS265246 抑制CDK4/cycD 活性，IC50为0.23 μM，抑制A2780 Cytox，IC50为0.76 μM。BMS265246 与CDK2结合，抑制位点与ATP嘌呤结合位点重合，且在蛋白骨架上与Leu83形成重要的氢键。BMS265246有效抑制CDK1和CDK2。BMS265246代表了最有力的CDK/CDK2选择性类似物。[1] | |||
|---|---|---|---|---|
| 激酶实验 | CDK1/Cyclin B1 激酶实验 | |||
| 激酶反应含 100 ng表达 GST-CDK1/cyclin B1 复合体的杆状病毒, 1 μg 组蛋白 H1, 0.2 μCi 33 P γ-ATP, 25 μM ATP，溶于50 μL 激酶 buffer中 (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT)。在 30oC下反应进行45分钟，然后加入三氯乙酸 (TCA)终止反应，终浓度为15%。使用 Filtermate 通用收集器，收集TCA 沉淀物到GF/C 联合过滤板上，使用TopCount 96 孔液体闪烁计数器测量过滤器。获得剂量反应曲线，测定抑制50%激酶活性 (IC50)所需的浓度。BMS265246溶于DMSO ，浓度为10 mM，按6种浓度估量，每种重复三次。实验中DMSO终浓度为2%。通过非线性回归分析测定IC50值，变异系数(SD/平均值, n = 6) 为16%。 | ||||
| 细胞实验 | 细胞系 | HCT116 | ||
| 浓度 | 0-5 μM | |||
| 孵育时间 | 24小时 | |||
| 方法 | HCT-116细胞接种在96孔板上。每孔中,通过计算每个视野领域的细胞数而测量细胞密度。细胞密度转化为相对于DMSO处理板平均细胞密度的相对百分比（即100％对应于DMSO处理的细胞平均密度）。使用TIBCO Spotfire拟合Logistic回归曲线,曲线为 50%时的浓度记为BMS-265246的EC50值。 | |||
化学信息&溶解度
| 分子量 | 345.34 | 分子式 | C18H17F2N3O2 |
| CAS号 | 582315-72-8 | SDF | Download BMS-265246 SDF |
| Smiles | CCCCOC1=C(C=NC2=NNC=C12)C(=O)C3=C(C=C(C=C3F)C)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 17 mg/mL ( (49.22 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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