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BMS-265246
BMS-265246是一種有效的選擇性CDK1/2抑制劑，無細胞試驗中IC50為6 nM/9 nM。作用于CDK1/2 比作用于CDK4選擇性高25倍。
BMS-265246 Chemical Structure
CAS: 582315-72-8
產(chǎn)品質(zhì)控
批次：
純度：
99.79%
99.79
BMS-265246相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | BMS-265246是一種有效的選擇性CDK1/2抑制劑，無細胞試驗中IC50為6 nM/9 nM。作用于CDK1/2 比作用于CDK4選擇性高25倍。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | BMS265246 抑制CDK4/cycD 活性，IC50為0.23 μM，抑制A2780 Cytox，IC50為0.76 μM。BMS265246 與CDK2結(jié)合，抑制位點與ATP嘌呤結(jié)合位點重合，且在蛋白骨架上與Leu83形成重要的氫鍵。BMS265246有效抑制CDK1和CDK2。BMS265246代表了最有力的CDK/CDK2選擇性類似物。[1] | |||
|---|---|---|---|---|
| 激酶實驗 | CDK1/Cyclin B1 激酶實驗 | |||
| 激酶反應(yīng)含 100 ng表達 GST-CDK1/cyclin B1 復(fù)合體的桿狀病毒, 1 μg 組蛋白 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下反應(yīng)進行45分鐘，然后加入三氯乙酸 (TCA)終止反應(yīng)，終濃度為15%。使用 Filtermate 通用收集器，收集TCA 沉淀物到GF/C 聯(lián)合過濾板上，使用TopCount 96 孔液體閃爍計數(shù)器測量過濾器。獲得劑量反應(yīng)曲線，測定抑制50%激酶活性 (IC50)所需的濃度。BMS265246溶于DMSO ，濃度為10 mM，按6種濃度估量，每種重復(fù)三次。實驗中DMSO終濃度為2%。通過非線性回歸分析測定IC50值，變異系數(shù)(SD/平均值, n = 6) 為16%。 | ||||
| 細胞實驗 | 細胞系 | HCT116 | ||
| 濃度 | 0-5 μM | |||
| 孵育時間 | 24小時 | |||
| 方法 | HCT-116細胞接種在96孔板上。每孔中,通過計算每個視野領(lǐng)域的細胞數(shù)而測量細胞密度。細胞密度轉(zhuǎn)化為相對于DMSO處理板平均細胞密度的相對百分比（即100％對應(yīng)于DMSO處理的細胞平均密度）。使用TIBCO Spotfire擬合Logistic回歸曲線,曲線為 50%時的濃度記為BMS-265246的EC50值。 | |||
化學(xué)信息&溶解度
| 分子量 | 345.34 | 分子式 | C18H17F2N3O2 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 17 mg/mL ( (49.22 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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