帕博西尼 T1785
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 571190-30-2 | ¥398.00 | 询底价 |
50 mg | 571190-30-2 | ¥754.00 | 询底价 |
10 mg | 571190-30-2 | ¥519.00 | 询底价 |
100 mg | 571190-30-2 | ¥869.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Palbociclib
描述: Palbociclib (PD 0332991) 是一种 CDK 抑制剂,抑制 CDK4 和 CDK6 (IC50=11/16 nM),具有口服活性。Palbociclib 具有抗肿瘤活性,有用于 ER 阳性和 HER2 阴性乳腺癌的研究潜力。
细胞实验: Palbociclib (PD) is prepared in DMSO and stored (?80°C), and then diluted with appropriate media before use[1]. MRT cell lines, G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) cell lines are seeded in normal growth medium into 96-well cell plates. After 24 h, the culture medium is replaced with culture medium containing Palbociclib (0.05 or 1 μM) or DMSO. Cells are cultured and treated in triplicate. Cell proliferation is determined 8 days after the treatment by WST-8 assay using a Cell Counting Kit-8.
激酶实验: CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792-928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and Palbociclib (0.001-0.1 μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25°C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4°C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.
体外活性: 方法:恶性横纹肌样瘤细胞 G401、MP-MRT-AN (AN)、KP-MRT-RY (RY)、KP-MRT-NS (NS) 和 KP-MRT-YM (YM) 用 Palbociclib (0-1 mM) 处理 24 h,使用 WST 方法检测细胞活力。结果:Palbociclib 以浓度依赖性的方式有效抑制 AN、RY、G401 和 NS 细胞系,IC50 分别为 0.01 μM、0.01 μM,0.06 μM 和 0.6 μM。相反,YM 细胞系对 Palbociclib 具有抗性,IC50>10 μM。[1]方法:人乳腺癌细胞 MDA-MB-453 用 Palbociclib (0.02-10 μmol/L) 处理 24 h,使用 Flow Cytometry 方法检测细胞周期情况。结果:Palbociclib 导致 G1 期阻滞。[2]
体内活性: 方法:为检测体内抗肿瘤活性,将 Palbociclib (12.5-150 mg/kg,sodium lactate buffer (50 mmol/L, pH 4.0)) 口服给药给携带肿瘤 Colo-205 或 MDA-MB-435 的免疫缺陷小鼠,每天一次,持续十四天。结果:Palbociclib 对多种人类肿瘤异种移植物模型显示出显著的抗肿瘤功效。对 Colo-205 肿瘤,PD 0332991 给药 14 天,可产生快速的肿瘤消退。[2]方法:为检测体内抗肿瘤活性,将 Palbociclib (150 mg/kg,sodium lactate buffer (50 mM, pH = 4.0)) 灌胃给药给携带食道鳞状细胞癌 (ESCC) 肿瘤 EC109 或 KYSE150 的 nu/nu BALB/c 小鼠,每天一次,持续两周。结果:Palbociclib 有效抑制 ESCC 肿瘤生长和肺转移。[3]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : < 1mg/ml (insoluble)
关键字: CDK | PD-0332991 | estrogen receptor | HER2 | HCC | inhibit | Inhibitor | Cyclin dependent kinase | hepatocellular carcinoma | cell cycle | PD0332991 | Breast cancer | Palbociclib
相关产品: MLS-573151 | Butyrolactone I | Lerociclib dihydrochloride | XL413 | 1-NM-PP1 | bio-THZ1 | P18IN011 | Samuraciclib hydrochloride | Isoangustone A | AT7519
相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Target-Focused Phenotypic Screening Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途