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Palbociclib isethionate

(Synonyms: PD 0332991 isethionate)
241 Cited Publications
Revisión del cliente

Based on 241 publication(s) in Google Scholar

Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate 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.

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  • Pureza: 99.98%
  • No. CAS: 827022-33-3
  • Fòrmula: C26H35N7O6S
  • Peso molecular:573.66
  • Almacenamiento:

    4°C, sealed storage, away from moisture

    * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

  • Palbociclib isethionate Chemical Structure
    Palbociclib isethionate Chemical Structure
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
  • Experimental Validation Results for Palbociclib isethionate
No. CAS: 827022-33-3
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  • Palbociclib isethionate Chemical Structure
    Palbociclib isethionate Chemical Structure
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    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Combined Palbociclib- and Fulvestrant-resistant cells, M-S and T-S, and the corresponding resistant cells, MPF-R and TPF-R, were treated with different inhibitors of the PI3K/AKT/mTOR pathway including Alpelisib (HY-15244; Alp; 1 μM in M-S/MPF-R and 250 to 500 nM in T-S/TPF-R), Capivasertib (Cap; 250 to 500 nM in M-S/MPF-R and 100 nM in T-S/TPF-R), Sapanisertib (Sap; 10 nM in M-S/MPF-R and 5 nM in T-S/TPF-R), and Gedatolisib (HY-10681; Ged; 10 nM) in combination with Palbociclib (HY-50767; Palbo; 200 nM) and Fulvestrant (HY-13636; Fulv; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Combined Palbociclib- and Fulvestrant-resistant cells (wild type ER+ breast cancer cells), ZPF-R, and the corresponding sensitive cells, Z-S, were treated with different inhibitors of PI3K/AKT/mTOR including Alpelisib (HY-15244; 6 μM), Capivasertib (50 nM), Sapanisertib (5 nM), and Gedatolisib (HY-10681; 5 nM) in combination with Palbociclib (HY-50767; 150 nM) and Fulvestrant (HY-13636; 100 nM) (n = 3 independent biological replicates per group, performed in duplicates).

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Dec 17;17(829):eadp5088. [Abstract]

    Customer Validation
     Triple combination with Gedatolisib (HY-10681), Palbociclib (HY-50767), and Fulvestrant (HY-13636) effectively inhibits growth of PIK3CA-mutant ER+ tumor xenografts resistant to combined palbociclib and fulvestrant. MPF-R cells (1 × 106) resistant to combined palbociclib and fulvestrant were injected into the mammary fat pads of NOG CIEA mice, and tumors were allowed to establish for 2 weeks to a size of ≈30 mm3. Mice were then treated with the combination of Fulvestrant (100 mg/kg, sc weekly), Palbociclib (25 mg/kg, oral gavage daily), and Capivasertib (100 mg/kg, oral gavage daily; n = 6) or Alpelisib (HY-15244; 25 mg/kg, oral gavage daily; n = 5). Tumor size was measured weekly. Average tumor growth curves measured weekly and Tumor volumes measured after excision.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Feb 16;15(1):1442. [Abstract]

    Customer Validation
     Palbociclib (50 nM; 4 h) effectively blocks S1900 phosphorylation of CAD in both KSHV de novo-infected human oral keratinocytes (HOKs) and KSHV-positive BCBL-1 lymphoma cells.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Aug 13:e2400666. [Abstract]

    Customer Validation
     Palbociclib (PD) (0.5 µM; 24 h) induces the interaction between CDK6 and AMBRA1/CUL4A, but not LC3B, in H69AR cells.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: bioRxiv. 2024 Nov 15:2024.11.11.623139. [Abstract]

    Customer Validation
     Continuous Palbociclib (1 μM) and fulvestrant (500 nM) treatment for 20 days significantly reduced resistant-cell growth compared to palbociclib discontinuation, fulvestrant alone, or fulvestrant plus INX-315 (100 nM).

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2023 Oct 2;83(19):3237-3251. [Abstract]

    Customer Validation
     Palbociclib (100 nM) inhibits cell growth in YFP control cells treated with E2 and ESR1-e6>YAP1, as well as in cells expressing ESR1-TAFs (SOX, ARNT2, and LPP) and two ERα LBD point mutants. The inhibitory effect on cells is significantly enhanced when combined with Pralsetinib (HY-112301) (500 nM).

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Dev Cell. 2023 Oct 9;58(19):1967-1982.e8. [Abstract]

    Customer Validation
     Palbociclib (PB) (1 μM; 24 h) reduces RB phosphorylation in SK-N-BE(2)C, IMR-32, and SH-SY5Y cells.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Dev Cell. 2023 Oct 9;58(19):1967-1982.e8. [Abstract]

    Customer Validation
     Palbociclib (PB) (1 μM; 5 days) significantly reduces proliferation in SK-N-BE(2)C, IMR-32, and SH-SY5Y cells.
    (B–D) Representative fluorescent images of EdU incorporation following a 24-h pulse in (B) SK-N-BE(2)C, (C) IMR-32, and (D) SH-SY5Y cells (pulse began day 4 of 5-day treatment with vehicle [DMSO] or palbociclib [1 μM]). Scale bars: 100 μm. Analysis of % cells with EdU incorporation. n = 3 biological replicates, mean ± SEM. ∗∗p ≤ 0.01, one-tailed paired t test. DAPI nuclear counters

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121652. [Abstract]

    Customer Validation
     Palbociclib (1 µM; 48 h) decreases the expression of PPARγ in SVFs.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

    Customer Validation
     The efficacy of Fulvestrant (Fulv, 100 nM), CDK4/6 inhibitor (CDK4/6i) Palbociclib (Palbociclib isothiocyanate; 200 nM) and the dual PI3K/mTOR inhibitor (PI3K/mTORi) Gedatolisib (10 nM) as single agents or in double and triple combination, was assessed in M-S and MPF-R cells by crystal violet growth assay performed over 6 days.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

    Customer Validation
     The efficacy of Fulvestrant (Fulv, 100 nM), CDK4/6 inhibitor (CDK4/6i) Palbociclib (Palbociclib isothiocyanate; 200 nM) and the dual PI3K/mTOR inhibitor (PI3K/mTORi) Gedatolisib (10 nM) as single agents or in double and triple combination, was assessed in T-S and TPF-R cells by crystal violet growth assay performed over 6 days.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]

    Customer Validation
     MPF-R and TPF-R cells were treated with different concentrations of the CDK4/6 inhibitor (CDK4/6i) Palbociclib (HY-A0065), Ribociclib (HY-15777C) or Abemaciclib (HY-16297A) for 6 days. Cell growth was measured by crystal violet colorimetric assay. Growth relative to vehicle (%) is plotted against log drug concentration.

  • 1/16

    Palbociclib isethionate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2021 Apr 1;27(7):1855-1863. [Abstract]

    Customer Validation
     Palbociclib (100-500 nM) significantly inhibits cell growth in MCF7 cells and demonstrates a robust additive cytostatic effect when administered 6 hours post-radiotherapy.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

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

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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