化合物 JNJ7706621|T6126|TargetMol

JNJ-7706621
443797-96-4

￥442 1mg 起订

￥638 2mg 起订

￥1130 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 JNJ7706621

英文名称：: JNJ-7706621

CAS号：: 443797-96-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.66%

产品类别：: 抑制剂

货号：: T6126

Product Introduction

Bioactivity

名称	JNJ-7706621
描述	JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2.
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.
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.
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
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。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 55 mg/mL (139.47 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	Cyclin dependent kinase \| CDK \| Apoptosis \| JNJ7706621 \| inhibit \| Inhibitor \| Aurora Kinase \| JNJ-7706621
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相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 抗癌化合物库 \| 已知活性化合物库 \| 细胞周期化合物库 \| 抗胰腺癌化合物库 \| 激酶抑制剂库 \| 含氟化合物库 \| 抗衰老化合物库

JNJ 7706621|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务