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

Palbociclib isethionate (Synonyms: PD 0332991 isethionate)

Cat. No.: HY-A0065 Purity: 99.96%
Handling Instructions

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

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

Palbociclib isethionate Chemical Structure

Palbociclib isethionate Chemical Structure

CAS No. : 827022-33-3

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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Palbociclib isethionate:

Top Publications Citing Use of Products

    Palbociclib isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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 isethionate 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

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    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    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 exhibits absolute selectivity for CDK4/6 with little or no activity against other CDKs. Palbociclib is effective at reducing Rb phosphorylation at Ser780 and Ser795 in MDA-MB-435 breast carcinoma cells with IC50 of 66 nM and 63 nM, respectively. Palbociclib is a potent inhibitor of cell growth and suppresses DNA replication by preventing cells from entering S phase. Palbociclib inhibits thymidine incorporation into the DNA of Rb-positive human breast (such as MDA-MB-435, MCF-7), colon (H1299), and lung carcinomas (Colo-205) as well as human leukemias (CRRF-CEM and K562), with IC50 values ranging from 0.04-0.17 μM. Palbociclib significant increases the percentage of MDA-MB-453 in G1 period[1]. Palbociclib inhibits phosphorylation of Rb in cycling CD138+ primary bone marrow myeloma cells, nontransformed primary B cells, MM1.S and CAG HMCLs cells line with IC50 of <0.1 μM, 0.05 μM, and 60-70 nM, respectively. Palbociclib treatment also induces G1 arrest of CD138+ primary bone marrow myeloma and nontransformed primary B cells. Palbociclib induces G1 arrest in MM1.S with IC50 of appr 0.05 μM[2]. Palbociclib preferentially inhibits proliferation of luminal estrogen receptor-positive (including HER2-positive) human breast cancer cell lines. Palbociclib increases gene expression of pRb and cyclin D1 and decreases gene expression of CDKN2A (p16) in most sensitive lines. Palbociclib enhances sensitivity to tamoxifen in cell lines with conditioned resistance to ER blockade[3]

    In Vivo

    Palbociclib(150 mg/kg. p.o.) produces rapid Colo-205 colon carcinoma xenografts regressions and a corresponding tumor growth delay. Palbociclib (150 mg/kg, p.o.) induces complete tumor stasis and cell kill in MDA-MB-435 breast carcinoma. Palbociclib (150 mg/kg) also induces significant tumor regression in mice bearing the SF-295 glioblastoma xenografts, and in ZR-75-1 breast and PC-3 prostate tumor models (complete suppression of tumor growth). Palbociclib (150 mg/kg) suppresses Rb Ser780 phosphorylation in MDA-MB-435 breast carcinoma over the full 24-hour period. Palbociclib (150 mg/kg) down-regulates expression of four E2F-regulated genes CDC2, CCNE2, TK1, and TOP2A in Colo-205 carcinoma xenografts[1]. Palbociclib also rapidly inhibits myeloma tumor growth[2]

    Clinical Trial
    Molecular Weight

    573.66

    Formula

    C₂₆H₃₅N₇O₆S

    CAS No.

    827022-33-3

    SMILES

    CC(C1=C(N2C3CCCC3)N=C(NC4=NC=C(N5CCNCC5)C=C4)N=C1)=C(C(C)=O)C2=O.OCCS(O)(=O)=O

    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: 

    H2O : ≥ 66.66 mg/mL (116.20 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7432 mL 8.7160 mL 17.4319 mL
    5 mM 0.3486 mL 1.7432 mL 3.4864 mL
    10 mM 0.1743 mL 0.8716 mL 1.7432 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [3]

    Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of Palbociclib are added. Control wells without drug are also seeded. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter Z2 particle counter.

    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 (appr 30 mg) into the region of the right axilla. Treatment is initiated when tumors reach 100 to 150 mg. Palbociclib 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: 99.96%

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    Product Name:
    Palbociclib isethionate
    Cat. No.:
    HY-A0065
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