化合物 PHA-793887|T2113|TargetMol

PHA-793887
718630-59-2

￥289 1mg 起订

￥413 2mg 起订

￥745 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 PHA-793887

英文名称：: PHA-793887

CAS号：: 718630-59-2

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：: 99.19%

产品类别：: 抑制剂

货号：: T2113

Product Introduction

Bioactivity

名称	PHA-793887
描述	PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.
细胞实验	Cells are seeded into 96- or 384-wells plates at final concentration ranging from 1 × 104 to 3 × 104 per cm2. After 24 hours, cells are treated using serial dilution of PHA-793887. At 72 hours after the treatment, the amount of cells are evaluated using the CellTiter-Glo assay. IC50 values are calculated using a sygmoidal fitt(Only for Reference)
激酶实验	CDK Kinase Assay: The biochemical activity of compounds is determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylated product. PHA-793887 (1.5 nM–10 μM) is incubated for 30?90 min at room temperature in the presence of ATP/33P-γ-ATP mix, substrate, and the specific enzyme (0.7?100 nM) in a final volume of 30 μL of kinase buffer, using 96 U bottom plates. After incubation, the reaction is stopped and the phosphorylated substrate is separated from nonincorporated radioactive ATP using SPA beads, Dowex resin, or Multiscreen phosphocellulose filter as follows: (1) For SPA Assays. The reaction is stopped by the addition of 100 μL of PBS + 32 mM EDTA + 0.1% Triton X-100 + 500 μM ATP, containing 1 mg of streptavidin-coated SPA beads. After 20 min of incubation for substrate capture, 100 μL of the reaction mixture is transferred into Optiplate 96-well plates containing 100 μL of 5 M CsCl, left to stand for 4 hours to allow stratification of beads to the top of the plate, and counted using TopCount to measure substrate-incorporated phosphate. (2) For Dowex Resin Assay. An amount of 150 μL of resin/formate, pH 3.00, is added to stop the reaction and capture unreacted 33P-γ-ATP, separating it from the phosphorylated substrate in solution. After 60 min of rest, 50 μL of supernatant is transferred to Optiplate 96-well plates. After the additon of 150 μL of Microscint 40, the radioactivity is counted in the TopCount. (3) For Multiscreen Assay. The reaction is stopped with the addition of 10 μL of EDTA (150 mM). An amount of 100 μL is transferred to a MultiScreen plate to allow substrate binding to phosphocellulose filter. Plates are then washed three times with 100 μL of H2PO4 (75 mM) filtered by a MultiScreen filtration system, and dried. After the additon of 100 μL of Microscint 0, radioactivity is counted in the TopCount. IC50 values are obtained by nonlinear regression analysis.
体外活性	20 mg/kg PHA-793887对携带K562和HL60细胞的移植瘤模型,原代白血病扩散细胞模型和复发Philadelphia-阳性急性淋巴性白血病患者高负荷播散性ALL-2模型有效.PHA-793887（10-30 mg/kg）在人卵巢A2780,结肠HCT-116和胰腺BX-PC3癌异种移植模型中显示出良好的功效.
体内活性	PHA-793887诱导细胞周期停滞,抑制Rb和核磷酸磷酸化,0.2-1 μM时调节细胞周期蛋白E和cdc6表达,5 μM时诱导凋亡。PHA-793887对白血病细胞系（包括K562,KU812,KCL22和TOM1）具有细胞毒性,IC50为0.3-7 μM,但对正常未刺激的外周血单个核细胞或CD34 +造血干细胞没有细胞毒性。PHA-793887作用于白血病细胞系具有高活性,IC50< 0.1 μM。 PHA-793887抑制许多肿瘤细胞系（包括A2780,HCT-116,COLO-205,C-433,DU-145,A375,PC3,MCF-7和BX-PC3）的细胞增殖,IC50为88 nM- 3.4 μM。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 67 mg/mL (185.3 mM) DMSO : 55 mg/mL (152.15 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	Inhibitor \| inhibit \| Apoptosis \| Cyclin dependent kinase \| CDK \| PHA-793887
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PHA793887|||PHA 793887|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)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
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