1. Cell Cycle/DNA Damage
  2. CDK
  3. Palbociclib

Palbociclib  (Synonyms: PD 0332991)

Cat. No.: HY-50767 Purity: 99.95%
COA Handling Instructions

Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

For research use only. We do not sell to patients.

Palbociclib Chemical Structure

Palbociclib Chemical Structure

CAS No. : 571190-30-2

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Customer Review

Based on 104 publication(s) in Google Scholar

Other Forms of Palbociclib:

Top Publications Citing Use of Products

95 Publications Citing Use of MCE Palbociclib

WB
IHC

    Palbociclib purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363.  [Abstract]

    LAPC-4 cells are grown in charcoal-stripped serum medium (CSS) for 24 hours and then stimulated by R1881 alone or with different doses of Palbociclib (PD). Palbociclib is added 30 min before androgen treatment. Cellular expression of all proteins is detected by immunoblotting analysis. β-actin is included as a control for protein loading.

    Palbociclib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 20;37(1):233.  [Abstract]

    Western blot of the nine cell cycle-related proteins in C666-1 cells treated with different concentrations of GEM (0.1, 1, and 10 μM) and PAL (0.1, 1, and 5 μM) after 48 h.

    Palbociclib purchased from MCE. Usage Cited in: Nat Commun. 2018 Oct 9;9(1):4180.  [Abstract]

    MCF7, MCF7-LEM4, and MCF7-TAMR cells are treated with 5% DCC-FBS (vehicle), 4-OHT (1 μM), PD0332991 (PD) (0.2 μM), or a combination of 4-OHT and PD0332991. Immunoblots of lysates from cells are tested.

    Palbociclib purchased from MCE. Usage Cited in: EBioMedicine. 2019 May;43:225-237.  [Abstract]

    Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with AZD2281 and Palbociclib either as single-agents or in combination for 4 days.

    Palbociclib purchased from MCE. Usage Cited in: Nature. 2017 Jun 15;546(7658):426-430.  [Abstract]

    In vitro kinase reactions using immunoprecipitated endogenous CDK6 and recombinant PFKP or PKM2 with or without Palbociclib (PALBO). 32P-PFKP and 32P-PKM2 denote phosphorylated proteins, IB, immunoblotting.

    Palbociclib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

    Palbociclib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

    Palbociclib purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.  [Abstract]

    Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

    Palbociclib purchased from MCE. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22.  [Abstract]

    Head-to-head comparison of the effect of Palbociclib and Ribociclib on DNA damage response (DDR) signalling in liver cancer cells.
    • Biological Activity

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    • References

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    Description

    Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma[1][3][4].

    IC50 & Target[1]

    Cdk4/cyclin D3

    9 nM (IC50)

    Cdk4/cyclin D1

    11 nM (IC50)

    Cdk6/cyclin D2

    16 nM (IC50)

    DYRK1A

    2000 nM (IC50)

    MAPK

    8000 nM (IC50)

    In Vitro

    Palbociclib (0-1 μM, 24 h) inhibits Rb Phosphorylation at Ser795 in MDA-MB-435 cells with an IC50 value of 0.063 μM, and obtains similar effects on both Ser780 and Ser795 phosphorylation in the Colo-205 colon carcinoma[1].
    Palbociclib (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase[1].
    Palbociclib (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
    Palbociclib (0-1 μM, 6 days) inhibits growth of several luminal ER-positive as well as HER2-amplified breast cancer cell lines, with IC50 values ranging from 4 nM to 1 μM[3].
    Palbociclib (0-1 μM, 3 days) inhibits the proliferation of human liver cancer cell lines with IC50 values ranging from 0.01 μM to 3.49 μM, and induces a reversible cell cycle arrest[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Cycle Analysis[1]

    Cell Line: MDA-MB-453 cells
    Concentration: 0-1 μM
    Incubation Time: 24 h
    Result: Arrested MDA-MB-453 cells in G1.

    Cell Proliferation Assay[3]

    Cell Line: ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
    Concentration: 0-1 μM
    Incubation Time: 6 days
    Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.
    In Vivo

    Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) produces rapid tumor regressions and delays tumor growth[1].
    Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) reduces Treg numbers and the Treg:CD8 ratio in the spleen and lymph nodes in tumor-free mice, demonstrating the tumor-independent effects[2].
    Palbociclib (oral administration, 100 mg/kg, daily for 1 week) has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
    Dosage: 75, 150 mg/kg, daily for 14 days
    Administration: Oral adminstration
    Result: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.
    Animal Model: Tumor-free female FVB mice[2]
    Dosage: 90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
    Administration: Oral adminstration
    Result: Reduced total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes.
    Animal Model: Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)[4]
    Dosage: 100 mg/kg, daily for 1 week.
    Administration: Oral adminstration
    Result: Decreased the luminescence signal in liver and delayed tumour growth.
    Clinical Trial
    Molecular Weight

    447.53

    Formula

    C24H29N7O2

    CAS No.
    SMILES

    O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (55.86 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)

    0.1 M HCL : 25 mg/mL (55.86 mM; ultrasonic and adjust pH to 4 with 0.1 M HCL)

    H2O : 0.1 mg/mL (0.22 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2345 mL 11.1724 mL 22.3449 mL
    5 mM 0.4469 mL 2.2345 mL 4.4690 mL
    10 mM 0.2234 mL 1.1172 mL 2.2345 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.96%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Palbociclib
    Cat. No.:
    HY-50767
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