Catalog No. A8316

PD 0332991 (Palbociclib) HCl

Name: PD 0332991 (Palbociclib) HCl,帕博西尼,Palbociclib monohydrochloride,827022-32-2
Brand: APExBIO
SKU: A8316
Price: 212 CNY
Availability: InStock

（别名：Palbociclib monohydrochloride, 帕博西尼）

CDK4/6抑制剂

规格	价格	货期
1mg	￥212.00	现货
2mg	￥360.00	现货
5mg	￥454.00	现货
10mg	￥630.00	现货
25mg	￥818.00	现货

CAS号：827022-32-2纯度：99.95%

仅用于科研，不用于诊疗。未经明确授权不得转售。

021-55669583sales@apexbio.cnAPExBIO

特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phos binding reagent (Phosbind) acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰

HotStart™ 2X Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用生物相关数据质量控制操作说明产品引用文献摩尔浓度计算器

产品描述

PD-0332991是一种选择性的和可口服的细胞周期蛋白依赖性激酶4/6（CDK4/6）抑制剂，IC50值分别为11 nM和16 nM[1]。

PD-0332991是一种高特异性的CDK4/6抑制剂。在Rb阳性肿瘤细胞中，PD-0332991是一种有效的抗增殖剂，特异性地诱导G1期停滞。据报道，PD-0332991阻止人骨髓瘤异种移植物中肿瘤的生长，诱导原代骨髓细胞中G1期停滞[2]。

对PD-0332991在乳腺癌中的作用也进行了研究。PD-0332991引起ER阳性细胞系和10/16 个HER2扩增细胞系的生长抑制。100 nM的PD-0332991可以抑制三个更敏感细胞系中Rb的磷酸化，从而阻止细胞周期进程[2]。

参考文献：
[1] Ivan Diaz-Padilla, Lillian L. Siu and Ignacio Duran. Cyclin-dependent kinase inhibitors as potential targeted anticancer agents. Invest New Drugs. 2009, 27: 586–594.
[2] Richard S Finn, Judy Dering, Dylan Conklin, Ondrej Kalous, David J Cohen, Amrita J Desai, Charles Ginther, Mohammad Atefi, Isan Chen, Camilla Fowst, Gerret Los and Dennis J Slamon. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Research. 2009, 11: R77.

产品性质

物理外观	A solid
CAS号	827022-32-2
分子式	C₂₄H₃₀ClN₇O₂
分子量	483.99
小分子别名	Palbociclib monohydrochloride
化学名称	6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
溶解度	≥14.48 mg/mL in H2O; ≥2.42 mg/mL in DMSO; ≥2.79 mg/mL in EtOH with gentle warming and ultrasonic
SMILES	CC(C1=C(C)c2cnc(Nc(cc3)ncc3N3CCNCC3)nc2N(C2CCCC2)C1=O)=O.Cl
存储条件	-20°C
运输条件	蓝冰

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述	Palbociclib (PD-0332991) HCl是CDK4/6的抑制剂，IC50值为11 nM/16 nM。
靶点	CDK4/cyclin D1	CDK6/cyclin D2
生物活性数据	11 nM	16 nM

生物相关数据

质量控制

请选择批次查看:

纯度 = 99.95%

COA (Certificate Of Analysis)HPLC NMR (Nuclear Magnetic Resonance)MSDS (Material Safety Data Sheet)

操作说明

小分子化合物通用使用指南 Datasheet Datasheet

APExBIO 顾客使用本产品发表的 15 篇科研文献

1. Nicholas W Harper, Gavin A Birdsall, et al. "RNA Pol II inhibition activates cell death independently from the loss of transcription." Cell. 2025 Aug 14:S0092-8674(25)00856-6. PMID: 40818455

2. Irit Shapira-Netanelov, Olga Furman, et al. "Patient-Derived Gastric Cancer Assembloid Model Integrating Matched Tumor Organoids and Stromal Cell Subpopulations." Cancers (Basel). 2025 Jul 9;17(14):2287. PMID: 40723172

3. Gavin A Birdsall, Michael J Lee et al. "Comprehensive Analysis of Drug Response using the FLICK Assay." J Vis Exp. 2025 Jun 6:(220): PMID: 40549770

4. Nicholas W. Harper, Gavin A. Birdsall et al. "Pol II degradation activates cell death independently from the loss of transcription." bioRxiv. 2025 Jan 14:2024.12.09.627542. PMID: 39713309

5. Paula Carpintero-Fernández, Michela Borghesan, et al. "Genome wide CRISPR/Cas9 screen identifies the coagulation factor IX (F9) as a regulator of senescence." Cell Death Dis. 2022 Feb 19;13(2):163. PMID: 35184131

6. Schwartz, Hannah, et al. "In vitro Methods to Better Evaluate Drug Responses in Cancer." UMass Chan Medical School. September 8, 2022

7. Anca Nastase, Amit Mandal, et al. "Integrated genomics point to immune vulnerabilities in pleural mesothelioma." Sci Rep. 2021 Sep 27;11(1):19138. PMID: 34580349

8. Minghui Liu, Liyuan Cui, et al. "PD-0332991 combined with cisplatin inhibits nonsmall cell lung cancer and reversal of cisplatin resistance." Thorac Cancer. 2021 Mar;12(6):924-931. PMID: 33534964

9. Anca Nastase, Amit Mandal, et al. "Multiple therapeutic pathways in malignant mesothelioma identified by genomic mapping." medRxiv. March 30, 2020

10. Borghesan M, Fafián-Labora J, et al. "Small Extracellular Vesicles Are Key Regulators of Non-cell Autonomous Intercellular Communication in Senescence via the Interferon Protein IFITM3." Cell Rep. 2019 Jun 25;27(13):3956-3971.e6. PMID: 31242426

11. Gasset-Rosa F, Lu S, et al. "Cytoplasmic TDP-43 De-mixing Independent of Stress Granules Drives Inhibition of Nuclear Import, Loss of Nuclear TDP-43, and Cell Death." Neuron. 2019 Apr 17;102(2):339-357.e7. PMID: 30853299

12. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID: 30038713

13. Azimi A, Caramuta S, et al. "Targeting CDK2 overcomes melanoma resistanceagainst BRAF and Hsp90 inhibitors." Mol Syst Biol. 2018 Mar 5;14(3):e7858. PMID: 29507054

14. Yuan J, Jiang YY, et al. "Super-Enhancers Promote Transcriptional Dysregulation in Nasopharyngeal Carcinoma." Cancer Res. 2017 Dec1;77(23):6614-6626. PMID: 28951465

15. Ma Y, Walsh MJ, et al. "CRISPR/Cas9 Screens Reveal Epstein-Barr Virus-Transformed B Cell Host Dependency Factors." Cell Host Microbe.2017 May 10;21(5):580-591.e7. PMID: 28494239