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

Palbociclib hydrochloride  (Synonyms: PD-0332991 hydrochloride)

製品番号: HY-50767C 純度: 99.96%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 571189-11-2

容量 価格（税別） 在庫状況 数量
5 mg $60 在庫あり
10 mg $84 在庫あり
50 mg $108 在庫あり
100 mg $132 在庫あり
500 mg $312 在庫あり
1 g $480 在庫あり
2 g $818 在庫あり
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カスタマーレビュー

Based on 220 publication(s) in Google Scholar

Other Forms of Palbociclib hydrochloride:

Palbociclib hydrochloride 関連抗体

Top Publications Citing Use of Products

顧客検証

Cell Proliferation/Viability Assay
WB
In Vivo Efficacy Study
IHC
IF
IP

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

    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).

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

    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).

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

    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.

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

    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.

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

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

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

    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).

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

    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).

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

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

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

    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

    Palbociclib hydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121652.

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

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

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

    Palbociclib hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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.

    Palbociclib hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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 hydrochloride purchased from MedChemExpress. 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.

    CDK アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

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

    IC50 & Target[1]

    DYRK1A

    2000 nM (IC50)

    MAPK

    8000 nM (IC50)

    Cdk4/cyclin D3

    9 nM (IC50)

    Cdk4/cyclin D1

    11 nM (IC50)

    Cdk6/cyclin D2

    16 nM (IC50)

    体外実験

    Palbociclib (0-1 μM, 24 h) hydrochloride inhibits retinoblastoma 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) hydrochloride arrests MDA-MB-453 cells exclusively in G1 phase[1].
    Palbociclib (500 nM, 7 days) hydrochloride 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) hydrochloride 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) hydrochloride 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].

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

    Palbociclib hydrochloride 関連抗体

    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.

    Cell Cycle Analysissup>[1]

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

    Palbociclib (oral adminstration, 75 or 150 mg/kg, daily for 14 days) hydrochloride produces rapid tumor regressions and delays tumor growth[1].
    Palbociclib (oral adminstration, 90 mg/kg, daily for 12 days) hydrochloride 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) hydrochloride has potent antitumour effects in genetically engineered mosaic mouse model of liver cancer[4].

    MedChemExpress (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
    Administration: Oral administration; daily for 14 days
    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
    Administration: Oral administration; daily for 12 days
    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
    Administration: Oral administration; daily for 1 week
    Result: Decreased the luminescence signal in liver and delayed tumour growth.
    分子量

    514.99

    分子式

    C24H30ClN7O2
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C(C(C)=O)=C(C2=CN=C(N=C2N1C3CCCC3)NC4=CC=C(N5CCNCC5)C=N4)C.Cl.[37/20]
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    H2O : 9.09 mg/mL (17.65 mM; ultrasonic and warming and adjust pH to 2 with 1 M HCl and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9418 mL 9.7089 mL 19.4179 mL
    5 mM 0.3884 mL 1.9418 mL 3.8836 mL
    10 mM 0.1942 mL 0.9709 mL 1.9418 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    純度とドキュメンテーション

    純度: 99.96%

    COA (254 KB) HNMR (300 KB) RP-HPLC (256 KB) MS (179 KB)

    取扱説明書 (2659 KB)
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 1.9418 mL 9.7089 mL 19.4179 mL 48.5446 mL
    5 mM 0.3884 mL 1.9418 mL 3.8836 mL 9.7089 mL
    10 mM 0.1942 mL 0.9709 mL 1.9418 mL 4.8545 mL
    15 mM 0.1295 mL 0.6473 mL 1.2945 mL 3.2363 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Palbociclib hydrochloride Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

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      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.

    Keywords:

    Palbociclib571189-11-2PD-0332991PD0332991PD 0332991CDKCyclin dependent kinaseBreast cancerhepatocellular carcinomaHCCestrogen receptorERHER2cell cycleInhibitorinhibitorinhibit

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    製品名:
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