Name: PD 0332991 (Palbociclib) HCl
Price: 145.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    PD-0332991 is selective and oral inhibitor of cyclin-dependent kinase 4/6 with IC50 values of 11nM and 16nM, respectively for CDK4 and CDK6 [1].
    PD-0332991 is a highly specific inhibitor of CDK4/6. It is a potent anti-proliferative agent against Rb-positive tumor cells in vitro, subsequently inducing an exclusive G1 arrest. It has been reported to prevent tumor growth in disseminated human myeloma xenografts and induce G1 arrest in primary bone marrow cells [2].
    PD-0332991 is also studied in breast cancer. It causes growth inhibition of ER-positive cell lines and 10/16 HER2-amplified cell lines. 100nM PD-0332991 can inhibit the phosphorylation of Rb in three more sensitive cell lines, resulting in prevention of cell cycle progression [2].
    
    [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.
- Properties
  - Alternative Name
    
    PD0332991; PD-0332991; PD 0332991; 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
    
    CAS Number
    
    827022-32-2
    
    Molecular Formula
    
    C24H30ClN7O2
    
    Molecular Weight
    
    483.99
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥14.48 mg/mL in H2O; ≥2.42 mg/mL in DMSO; ≥2.79 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. 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
    2. 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
    3. Anca Nastase, Amit Mandal, et al. "Multiple therapeutic pathways in malignant mesothelioma identified by genomic mapping." medRxiv. March 30, 2020.
    4. 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
    5. 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
    6. 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
    7. Azimi A, Caramuta S, et al. "Targeting CDK2 overcomes melanoma resistance against BRAF and Hsp90 inhibitors." Mol Syst Biol. 2018 Mar 5;14(3):e7858. PMID:29507054
    8. Yuan J, Jiang YY, et al. "Super-Enhancers Promote Transcriptional Dysregulation in Nasopharyngeal Carcinoma." Cancer Res. 2017 Dec 1;77(23):6614-6626. PMID:28951465
    9. 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

PD 0332991 (Palbociclib) HCl

PD 0332991 (Palbociclib) HCl

Background

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