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    Palbociclib (PD-0332991) HCl
    Palbociclib (PD-0332991) HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1531
    CAS #: 827022-32-2 Purity ≥98%

    Description: Palbociclib HCl (Pfizer trade name Ibrance, also known as PD-0332991), the HCl salt of Palbociclib, is a highly selective, orally bioavailable pyridopyrimidine-derived inhibitor of CDK4/6 with potential antineoplastic activity. It inhibits CDK4 and CDK6 with IC50s of 11 nM and 16 nM in cell-free assays respectively. CDK4 and CDK6 are overexpressed in many tumor cells, and palbociclib, developed by Pfizer, is the first CDK4/6 inhibitor approved by FDA in 2017 as a cancer therapeutic. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. 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.

    References: Mol Cancer Ther. 2004 Nov;3(11):1427-38; Cancer Res. 2006 Aug 1;66(15):7661-7;  2018 Apr 18;9(5):446. ;  2018 Apr 18. pii: e98359. doi: 10.15252/embj.201798359.

    Related CAS#: 571190-30-2 (free base); 827022-33-3 (isethionate salt); 827022-33-3 (isethionate); 827022-32-2 (HCl); 1628752-83-9 (Palbociclib D8); 2366269-23-8 (Palbociclib-propargyl)

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    Molecular Weight (MW)483.99
    FormulaC24H29N7O2.HCl 
    CAS No.827022-32-2 (HCl salt); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 3 mg/mL (6.2 mM)
    Water: 30 mg/mL (62.0 mM)
    Ethanol:<1 mg/mL
    Solubility (In vivo)Saline: 20 mg/mL 
    Synonyms

    Palbociclib; PD-332991; PD332991; PD 332991; PD0332991; PD-0332991; PD0332991 HCl,  PD-0332991 hydrochloride; PD 0332991; Palbociclib HCl, Trade name: Ibrance

    Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride

    SMILES Code: O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5.[H]Cl


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    In Vitro

    In vitro activity: PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 μM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells. PD 0332991 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. A recent study shows that PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16.


    Kinase Assay: A stock solution of PD0332991 is prepared in DMSO. 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 PD 0332991 (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.


    Cell Assay: Cells (Tumor cell lines including MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM and K562) are seeded at 2 × 104 per well in a 96-well plate and incubated overnight. PD 0332991 (0.01-1 μM) is added to the wells and incubated at 37 °C for another 24 hours. [14C]Thymidine (0.1 μCi) is added to each well and incorporation of the radiolabel is allowed to proceed for 72 hours. Incorporated radioactivity is determined with a β plate counter.

    In VivoPD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F.
    Animal modelAdvanced stage human tumor xenografts including Colo-205, MDA-MB-435 breast, SF-295 glioblastoma, ZR-75-1 breast, PC-3 prostate, H125 lung, SW-620 colon, H23 lung and MDA-MB-468 breast (Rb negative) are established in severe combined immunodeficient mice.
    Formulation & DosageDissolved in sodium lactate buffer (50 mM, pH 4.0); ~150 mg/kg; Oral gavage
    References

    Mol Cancer Ther. 2004 Nov;3(11):1427-38.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Palbociclib (PD-0332991) HCl


    Evaluation of IC50 concentrations of the CDK inhibitors dinaciclib and palbociclib on proliferation, and their effects on CDK-Rb-E2F signaling in human HPASMCs from healthy donors and IPAH patients.  2019 May 17;10(1):2204.

     Palbociclib (PD-0332991) HCl


    Effects of the CDK inhibitors dinaciclib and palbociclib on proliferation, cell cycle, and apoptosis.  2019 May 17;10(1):2204.

     Palbociclib (PD-0332991) HCl


    Effects of palbociclib on disease progression in the MCT rat model of pulmonary arterial hypertension.  2019 May 17;10(1):2204.

     Palbociclib (PD-0332991) HCl


    Effects of palbociclib on disease progression in the Su/Hox rat model of pulmonary arterial hypertension.  2019 May 17;10(1):2204.

     Palbociclib (PD-0332991) HCl


    Ex vivo analyses of lung tissue for reversal of remodeling and in vivo drug efficacy in the Su/Hox model.  2019 May 17;10(1):2204.

     Palbociclib (PD-0332991) HCl


    Proposed mechanism of action of palbociclib and dinaciclib in PAH. Multiple growth factors, cytokines, and mitogens induce the activation of cyclin-dependent kinases (CDKs), e.g., by increasing the expression of cyclin D1.  2019 May 17;10(1):2204.

     

    Palbociclib (PD-0332991) HCl

     

    Palbociclib (PD-0332991) HCl

     

    Palbociclib (PD-0332991) HCl


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