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JNJ-7706621

JNJ-7706621

产品编号 T6126   CAS 443797-96-4
别名: JNJ 7706621

JNJ-7706621 是一种aurora kinase 抑制剂,有效抑制CDK1和CDK2,对CDK1,CDK2,aurora-A 和aurora-B 的IC50值分别为 9 nM,3 nM,11 nM 和 15 nM。

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JNJ-7706621 Chemical Structure
JNJ-7706621, CAS 443797-96-4
规格 价格/CNY 货期 数量
1 mg ¥ 442 现货
2 mg ¥ 638 现货
5 mg ¥ 1,130 现货
10 mg ¥ 1,980 现货
25 mg ¥ 2,970 现货
50 mg ¥ 4,530 现货
100 mg ¥ 6,350 现货
500 mg ¥ 12,900 现货
1 mL * 10 mM (in DMSO) ¥ 987 现货
产品目录号及名称: JNJ-7706621 (T6126)
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纯度: 99.66%
纯度: 99.1%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.
靶点活性 Aurora A:11 nM, Aurora B:15 nM, CDK2/CyclinE:3 nM, CDK2/CyclinA:4 nM, CDK1/CyclinB:9 nM
体外活性 JNJ-7706621(100或125 mg/kg)导致携带A375恶性黑色素瘤人类肿瘤移植瘤模型的小鼠中肿瘤消退.
体内活性 JNJ-7706621在抑制正常细胞类型(包括MRC-5,HASMC,HUVEC和HMVEC)的生长方面具有几倍的效力,IC50为3.67-5.42 μM。JNJ-7706621对CDK1和2具有高度有效性,IC50为3-9 nM。JNJ-7706621显示对包括HeLa,HCT-116,SK-OV-3,PC3,DU145,A375,MDA-MB-231,MES-SA和MES-SA/Dx5在内的一组人类癌细胞类型的抑制作用 ,IC50为112-514 nM,独立于p53,成视网膜细胞瘤或P-糖蛋白状态。JNJ-7706621也抑制CDK3,4和6,IC50为58-253 nM。JNJ-7706621抑制Aurora-A和B,IC50分别为11和15 nM。JNJ-7706621也抑制VEGF-R2,FGF-R2和GSK3β,IC50为154-254 nM。在HeLa或U937细胞中,JNJ-7706621(0.5-3 μM)延迟从G1期中退出,使细胞停滞在G2-M期,诱导核内复制,激活凋亡并减少集落形成。
激酶实验 In vitro kinase assay for CDK1 and Aurora kinases:CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.The Aurora kinase activity is measured with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.
细胞实验 Cell lines: HeLa,HCT-116,A375,SK-OV-3,MDA-MB-231 and PC-3 cells. Concentrations: 1 nM - 10 μM,dissolved in DMSO. Method: Measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells to determine the ability of JNJ-7706621 to inhibit the proliferation of cell growth.Cells are trypsinized and counted and 3-8 ×103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in 100 μL complete medium in a volume.Cells are incubated for 24 hours at 37 °C in an atmosphere containing 5% CO2.Next,1 μL JNJ-7706621 is added to the wells of the plate.Cells are incubated for another 24 hours.Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL.The plate is incubated for 24 hours at 37 °C in JNJ-7706621 with 14C-thymidine.The contents of the plate are discarded and the plate is washed twice with 200 μL PBS.200 μL of PBS is added to each well.The top of the plate is sealed with a transparent plate sealer and a white plate backing sealer is applied to the bottom of the plate.The degree of methyl 14C-thymidine incorporation is quantified on a Packard Top Count.
动物实验 Animal Models: Mouse xenograft model of A375 cellsFormulation & . Dosages: Dissolved in 0.5% methylcellulose containing 0.1% polysorbate 80 in sterile water.100 or 125 mg/kg. Administration: Orally or by intraperitoneal injection
别名 JNJ 7706621
分子量 394.36
分子式 C15H12F2N6O3S
CAS No. 443797-96-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 73 mg/mL (185.1 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5358 mL 12.6788 mL 25.3575 mL 63.3939 mL
5 mM 0.5072 mL 2.5358 mL 5.0715 mL 12.6788 mL
10 mM 0.2536 mL 1.2679 mL 2.5358 mL 6.3394 mL
20 mM 0.1268 mL 0.6339 mL 1.2679 mL 3.1697 mL
50 mM 0.0507 mL 0.2536 mL 0.5072 mL 1.2679 mL
100 mM 0.0254 mL 0.1268 mL 0.2536 mL 0.6339 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Emanuel S, et al. Cancer Res, 2005, 65(19), 9038-9046. 2. Seamon JA, et al. Mol Cancer Ther, 2006, 5(10), 2459-2467. 3. Lin R, et al. J Med Chem, 2005, 48(13), 4208-4211.
OTS964 hydrochloride CLK1/2-IN-3 SRX3177 CDK4-IN-1 (S)-Enitociclib HQ461 SHR5428 26-Deoxyactein

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 含氟化合物库 临床前化合物库 细胞凋亡化合物库 抗乳腺癌化合物库 表观遗传库 已知活性化合物库 抑制剂库 经典已知活性库 自噬库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

JNJ-7706621 443797-96-4 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic CDK Aurora Kinase Cyclin dependent kinase JNJ7706621 JNJ 7706621 inhibit Inhibitor inhibitor

 

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