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

Palbociclib hydrochloride (Synonyms: PD 0332991 hydrochloride)

Cat. No.: HY-50767A Purity: 99.94%
Handling Instructions

Palbociclib hydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively.

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

Palbociclib hydrochloride Chemical Structure

Palbociclib hydrochloride Chemical Structure

CAS No. : 827022-32-2

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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Palbociclib hydrochloride:

Top Publications Citing Use of Products

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

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

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

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

    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 hydrochloride purchased from MCE. Usage Cited in: Eur J Cancer. 2018 Oct;102:10-22.

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

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

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

    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 hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2018 Oct 9;9(1):4180.

    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 hydrochloride purchased from MCE. Usage Cited in: EBioMedicine. 2019 May;43:225-237.

    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.
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    Palbociclib hydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively.

    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

    The IC50 of Palbociclib (PD 0332991) for reduction of retinoblastoma (Rb) phosphorylation at Ser780 in MDA-MB-435 breast carcinoma cells is 66 nM. Palbociclib is equally effective at reducing Rb phosphorylation at Ser795 in this tumor with an IC50 of 63 nM, and similar effects on both Ser780 and Ser795 phosphorylation are obtained in the Colo-205 colon carcinoma[1]. The MP-MRT-AN (AN), KP-MRT-RY (RY), G401, and KP-MRT-NS (NS) cell lines are effectively inhibited by Palbociclib (PD) in a concentration-dependent manner in a WST-8 assay. The IC50s are 0.01 µM, 0.01 µM, 0.06 µM, and 0.6 µM, respectively. In contrast, the KP-MRT-YM (YM) cell line is resistant to Palbociclib (IC50>10 µM). The flow cytometry results show that Palbociclib at concentrations between 0 to 1.0 µM induces G1 arrest in the AN, RY, G401 and NS cell lines in a concentration-dependent manner, but has no effect on YM cells. The BrdU incorporation results are consistent with the WST-8 and flow cytometry results: PD reduces BrdU incorporation (indicating G1 arrest) in the AN, RY, G401 and NS cell lines, but not in the YM cell line. Palbociclib, even at a concentration of 0.05 µM, significantly reduces BrdU incorporation in the AN, RY, and G401 cell lines (p<0.05)[2].

    In Vivo

    Palbociclib (PD 0332991) exhibits significant antitumor efficacy against multiple human tumor xenograft models. In mice bearing Colo-205 colon carcinoma xenografts (p16 deleted), daily p.o. dosing for 14 days with Palbociclib (150 or 75 mg/kg) produces rapid tumor regressions and a corresponding tumor growth delay of ~50 days with >1 log of tumor cell kill at the highest dose tested. At 37.5 mg/kg, the tumor slowly regressed during treatment. Even at doses as low as 12.5 mg/kg, a 13-day growth delay is obtained indicating a 90% inhibition of tumor growth rate. Likewise, robust antitumor activity is seen in the MDA-MB-435 breast carcinoma (p16 deleted) where complete tumor stasis is apparent at 150 mg/kg and some cell kill is evident at the highest dose[1].

    Clinical Trial
    Molecular Weight

    483.99

    Formula

    C₂₄H₃₀ClN₇O₂

    CAS No.

    827022-32-2

    SMILES

    O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 5.4 mg/mL (11.16 mM; Need ultrasonic)

    H2O : 4.9 mg/mL (10.12 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0662 mL 10.3308 mL 20.6616 mL
    5 mM 0.4132 mL 2.0662 mL 4.1323 mL
    10 mM 0.2066 mL 1.0331 mL 2.0662 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.54 mg/mL (1.12 mM); Clear solution

    • 2.

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

      Solubility: ≥ 0.54 mg/mL (1.12 mM); Clear solution

    • 3.

      Add each solvent one by one:  Lactic acid buffer (50 mM, pH 4.0)

      Solubility: 33.33 mg/mL (68.87 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    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 (0.001-0.1μM). 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.

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

    Cell Assay
    [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.

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

    Animal Administration
    [1]

    Mice (18-22 g) are randomized and then implanted s.c. with tumor fragments (30 mg) into the region of the right axilla. Treatment is initiated when tumors reach 100 to 150 mg. PD 0332991 (150 or 75 mg/kg, p.o.) is given according to the schedule and dose indicated in the table and figure legends by gavage as a solution in sodium lactate buffer (50 mM, pH 4.0) based on mean group body weight. In all experiments, there are 12 mice in the control group and 8 mice each in the treated groups. Additional details for each experiment are given in the table legends.

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

    References

    Purity: 99.94%

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    Palbociclib hydrochloride
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