Palbociclib monohydrochloride
Based on 245 publication(s) in Google Scholar
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride 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.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 827022-32-2
- Formula: C24H30ClN7O2
- Molecular Weight:483.99
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Palbociclib monohydrochloride
More- Signal Transduct Target Ther. 2025 Dec 15;10(1):406. [Abstract]
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- JCI Insight. 2021 Apr 8;6(7):e139497. [Abstract]
- Ecotoxicol Environ Saf. 2020 Dec 1;205:111146. [Abstract]
- Cancer Cell Int. 2024 Dec 27;24(1):433. [Abstract]
- Int J Mol Med. 2025 Nov;56(5):167. [Abstract]
- Breast Cancer Res. 2024 Jun 7;26(1):95. [Abstract]
- Cell Prolif. 2023 Jan;56(1):e13337. [Abstract]
- Biochem Pharmacol. 2017 Jan 15:124:29-42. [Abstract]
- Mol Cancer Ther. 2025 Jul 2. [Abstract]
- Inflamm Res. 2023 Jun;72(6):1147-1160. [Abstract]
- Mar Drugs. 2020 Sep 27;18(10):494. [Abstract]
- Liver Int. 2026 Apr;46(4):e70582. [Abstract]
- Cells. 2023 Dec 30;13(1):81. [Abstract]
- J Pathol. 2023 Jun;260(2):203-221. [Abstract]
- Commun Biol. 2025 May 30;8(1):829. [Abstract]
- Life Sci. 2023 Jun 1:322:121652. [Abstract]
- Int J Mol Sci. 2023 Mar 12;24(6):5408. [Abstract]
- Int J Mol Sci. 2021 Mar 25;22(7):3367. [Abstract]
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- Biomolecules. 2025 Jun 16;15(6):873. [Abstract]
- Mol Cancer Res. 2018 Mar;16(3):361-377. [Abstract]
- Molecules. 2023 May 27;28(11):4380. [Abstract]
- Mol Oncol. 2023 Dec;17(12):2507-2525. [Abstract]
- Mol Oncol. 2017 Aug;11(8):1035-1049. [Abstract]
- Cancers (Basel). 2024 Aug 7;16(16):2785. [Abstract]
- Cancers (Basel). 2023 Mar 22;15(6):1908. [Abstract]
- Cancers (Basel). 2021 Mar 24;13(7):1494. [Abstract]
- Cancers. 2020 Jun 16;12(6):1596. [Abstract]
- Front Cell Dev Biol. 2020 Aug 31;8:843. [Abstract]
- J Cell Mol Med. 2021 Mar;25(6):3124-3135. [Abstract]
- Transl Oncol. 2025 Jan 3:52:102264. [Abstract]
- iScience. 2022 Sep 6;25(10):105081. [Abstract]
- J Cell Physiol. 2025 Nov;240(11):e70113. [Abstract]
- J Biol Chem. 2026 Jun;302(6):111461. [Abstract]
- Sci Rep. 2026 Jan 5;16(1):4751. [Abstract]
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- J Biol Chem. 2025 Jan 16:108196. [Abstract]
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- Sci Rep. 2024 May 8;14(1):10582. [Abstract]
- J Biol Chem. 2023 Dec;299(12):105407. [Abstract]
- J Biol Chem. 2023 Jun;299(6):104786. [Abstract]
- Sci Rep. 2023 Jan 31;13(1):1711. [Abstract]
- Sci Rep. 2021 Mar 8;11(1):5374. [Abstract]
- J Virol. 2023 Jun 29;97(6):e0037023. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Cell Signal. 2025 Jul:131:111709. [Abstract]
- Biochim Biophys Acta. 2017 Nov 20;1865(2):354-363. [Abstract]
- Development. 2023 May 1;150(9):dev200903. [Abstract]
- J Bone Oncol. 2021 Sep 20:30:100391. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Future Med Chem. 2019 Feb;11(3):165-177. [Abstract]
- Endocrinology. 2023 Aug 28;164(10):bqad135. [Abstract]
- Front Oncol. 2022 Apr 8;12:819003. [Abstract]
- Discov Oncol. 2025 May 19;16(1):814. [Abstract]
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- Leuk Res. 2022 Sep:120:106920. [Abstract]
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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IP
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WB
Biological Activity
|
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) |
Palbociclib monohydrochloride (0-1 μM, 24 h) inhibits Rb 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 monohydrochloride (0-10 μM, 24 h) arrests MDA-MB-453 cells exclusively in G1 phase[1].
Palbociclib monohydrochloride (500 nM, 7 days) increases expression of homologous genes (H2d1, H2k1, and B2m) in MDA-MB-453 and MDA-MB-361 cells[2].
Palbociclib monohydrochloride (0-1 μM, 6 days) 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 monohydrochloride (0-1 μM, 3 days) 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.
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Cell Line:MDA-MB-453 cells
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Concentration:0-1 μM
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Incubation Time:24 h
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Result:Arrested MDA-MB-453 cells in G1.
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Cell Line:ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc.)
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Concentration:0-10 μM
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Incubation Time:6 days
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Result:Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.
Palbociclib monohydrochloride (oral adminstration, 90 mg/kg, daily for 12 days) 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 monohydrochloride (oral administration, 100 mg/kg, daily for 1 week) 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.
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Animal Model:Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
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Dosage:75, 150 mg/kg, daily for 14 days
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Administration:Oral adminstration
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Result:Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days.
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Animal Model:Tumor-free female FVB mice[2]
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Dosage:90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days
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Administration:Oral adminstration
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Result:Reduced total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes.
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Animal Model:Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)[4]
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Dosage:100 mg/kg, daily for 1 week.
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Administration:Oral adminstration
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Result:Decreased the luminescence signal in liver and delayed tumour growth.
Chemical Information
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CAS No. 827022-32-2
-
Appearance Solid
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Molecular Weight 483.99
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Formula C24H30ClN7O2
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Color Light yellow to yellow
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SMILES
O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5.Cl
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Synonyms
PD 0332991 monohydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (245)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Nature
2020 Dec;588(7836):169-173. PMID: 33087935 -
Nature
2020 Jul;583(7817):620-624. PMID: 32669709 -
Nature
2017 Aug 24;548(7668):471-475. PMID: 28813415 -
Nature
2017 Jun 15;546(7658):426-430. PMID: 28607489
Palbociclib monohydrochloride 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.
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Cancer Cell
GABAergic neuronal lineage development determines clinically actionable targets in diffuse hemispheric glioma, H3G34-mutant. [Abstract]2024 Aug 27:S1535-6108(24)00305-2. PMID: 39232581 -
Cancer Cell
Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026 -
Cancer Cell
2017 Apr 10;31(4):576-590.e8. PMID: 28399412 -
Mol Cancer
Genome-wide in vivo CRISPR screen identifies TGFβ3 as actionable biomarker of palbociclib resistance in triple negative breast cancer. [Abstract]2024 Jun 3;23(1):118. PMID: 38831405 -
Mol Cancer
S6K1 amplification confers innate resistance to CDK4/6 inhibitors through activating c-Myc pathway in patients with estrogen receptor-positive breast cancer. [Abstract]2022 Aug 30;21(1):171. PMID: 36042494 -
Cancer Discov
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations. [Abstract]2024 Sep 13:OF1-OF20. PMID: 39269178 -
Nat Methods
2022 Mar;19(3):331-340. PMID: 35228726 -
Nat Cancer
IL-17A-secreting γδ T cells promote resistance to CDK4/CDK6 inhibitors in HR+HER2- breast cancer via CX3CR1+ macrophages. [Abstract]2025 Jul 7. PMID: 40624238 -
Nat Cancer
CDK4/6 inhibition reprograms the breast cancer enhancer landscape by stimulating AP-1 transcriptional activity. [Abstract]2021 Jan;2(1):34-48. PMID: 33997789 -
Nat Immunol
Cell cycle arrest enhances CD8+ T cell effector function by potentiating glucose metabolism and IL-2 signaling. [Abstract]2026 Mar;27(3):463-475. PMID: 41555086 -
Immunity
Mitochondrial DNA released by senescent tumor cells enhances PMN-MDSC-driven immunosuppression through the cGAS-STING pathway. [Abstract]2025 Apr 8;58(4):811-825.e7. PMID: 40203808 -
Nat Cell Biol
Electrophilic compound screening identifies GPX4-dependent ferroptosis as a senescence vulnerability. [Abstract]2026 May;28(5):915-929. PMID: 42032311 -
Nat Cell Biol
An SP110-SP100 axis is a critical regulator of promyelocytic leukaemia body dynamics and mitotic fidelity. [Abstract]2026 Mar 13. PMID: 41826696 -
Mol Cell
CDK4/6 inhibitor-mediated cell overgrowth triggers osmotic and replication stress to promote senescence. [Abstract]2023 Nov 16;83(22):4062-4077.e5. PMID: 37977118 -
Mol Cell
A fluorophore-conjugated reagent enabling rapid detection, isolation and live tracking of senescent cells. [Abstract]2023 Oct 5;83(19):3558-3573.e7. PMID: 37802028 -
Cancer Res
Targeting transcriptional regulation with a CDK9 inhibitor suppresses growth of endocrine- and palbociclib-resistant ER+ breast cancers. [Abstract]2024 Jan 2;84(1):17-25. PMID: 37801608 -
Cancer Res
Abemaciclib is effective in palbociclib-resistant hormone receptor-positive metastatic breast cancers. [Abstract]2023 Oct 2;83(19):3264-3283. PMID: 37384539 -
Cancer Res
2023 Oct 2;83(19):3237-3251. PMID: 37071495
Palbociclib monohydrochloride 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).
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Cancer Res
A Genome-Wide CRISPR Activation Screen Identifies PRRX2 as a Regulator of Enzalutamide Resistance in Prostate Cancer. [Abstract]2022 Jun 6;82(11):2110-2123. PMID: 35405009 -
Cancer Res
2021 Jan 1;81(1):187-198. PMID: 33122307 -
Mol Cell
Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer. [Abstract]2020 Jun 18;78(6):1096-1113.e8. PMID: 32416067 -
Cancer Res
2019 Oct 15;79(20):5245-5259. PMID: 31395606 -
Mol Cell
2017 Oct 19;68(2):336-349.e6. PMID: 29053957 -
ACS Nano
Senescence-Primed Ferroptosis Enabled by a Metal-Organic Framework Nanoplatform for Enhanced Cancer Therapy. [Abstract]2025 Dec 23;19(50):42689-42704. PMID: 41358603 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
CDK2 inhibitor BLU-222 synergizes with CDK4/6 inhibitors in drug resistant breast cancers through p21/p27 induction. [Abstract]2026 Jan 22;17(1):619. PMID: 41571637 -
Nat Commun
O-GlcNAcylation of FOXK1 co-opts BAP1 to orchestrate the E2F pathway and promotes oncogenesis. [Abstract]2025 Jul 1;16(1):5959. PMID: 40593803 -
Nat Commun
Attenuated growth factor signaling during cell death initiation sensitizes membranes towards peroxidation. [Abstract]2025 Feb 25;16(1):1774. PMID: 40000627 -
Nat Commun
Hijacking of nucleotide biosynthesis and deamidation-mediated glycolysis by an oncogenic herpesvirus. [Abstract]2024 Feb 16;15(1):1442. PMID: 38365882
Palbociclib monohydrochloride 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.
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Nat Commun
Oxidative phosphorylation is a metabolic vulnerability of endocrine therapy and palbociclib resistant metastatic breast cancers. [Abstract]2023 Jul 14;14(1):4221. PMID: 37452026 -
Nat Commun
Targeting the Retinoblastoma/E2F repressive complex by CDK4/6 inhibitors amplifies oncolytic potency of an oncolytic adenovirus. [Abstract]2022 Aug 10;13(1):4689. PMID: 35948546 -
Nat Commun
Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation. [Abstract]2021 Nov 16;12(1):6607. PMID: 34785661 -
Nat Commun
Co-targeting CDK4/6 and AKT with endocrine therapy prevents progression in CDK4/6 inhibitor and endocrine therapy-resistant breast cancer. [Abstract]2021 Aug 25;12(1):5112. PMID: 34433817
Palbociclib monohydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
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.
Palbociclib monohydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
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.
Palbociclib monohydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 25;12(1):5112. [Abstract]
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.
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Nat Commun
2021 Jul 22;12(1):4457. PMID: 34294701 -
Nat Commun
PLK1 inhibition exhibits strong anti-tumoral activity in CCND1-driven breast cancer metastases with acquired palbociclib resistance. [Abstract]2020 Aug 13;11(1):4053. PMID: 32792481 -
Nat Commun
Identification of predictors of drug sensitivity using patient-derived models of esophageal squamous cell carcinoma. [Abstract]2019 Nov 7;10(1):5076. PMID: 31700061 -
Nat Commun
LEM4 confers tamoxifen resistance to breast cancer cells by activating cyclin D-CDK4/6-Rb and ERα pathway. [Abstract]2018 Oct 9;9(1):4180. PMID: 30301939
Palbociclib monohydrochloride 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.
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Cell Death Differ
E2F and STAT3 provide transcriptional synergy for histone variant H2AZ activation to sustain glioblastoma chromatin accessibility and tumorigenicity. [Abstract]2022 Jul;29(7):1379-1394. PMID: 35058574 -
Cell Death Differ
ARID1A prevents squamous cell carcinoma initiation and chemoresistance by antagonizing pRb/E2F1/c-Myc-mediated cancer stemness. [Abstract]2020 Jun;27(6):1981-1997. PMID: 31831874 -
Neuron
Seeded aggregation of TDP-43 induces its loss of function and reveals early pathological signatures. [Abstract]2025 Mar 26:S0896-6273(25)00180-1. PMID: 40157355 -
Trends Biotechnol
Long-offset paired nicking-based efficient and precise strategy for in vivo targeted insertion. [Abstract]2025 Apr 7:S0167-7799(25)00083-6. PMID: 40199626 -
Sci Transl Med
Dual PI3K/mTOR inhibition is required to combat resistance to CDK4/6 inhibitor and endocrine therapy in PIK3CA-mutant breast cancer. [Abstract]2025 Dec 17;17(829):eadp5088. PMID: 41406241
Palbociclib monohydrochloride 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 monohydrochloride 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 monohydrochloride 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.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Adv Sci (Weinh)
Biomimetic Nanomedicine for Senescence-Modulated Immune Activation Enhances Immunotherapy Efficacy in Hepatocellular Carcinoma. [Abstract]2025 Dec 23:e17792. PMID: 41432006 -
Adv Sci (Weinh)
De Novo Gene Transcription of Connexin Mediates Cytoplasmic Fluid Exchange and Flocking Transitions in Physiological and Cancerous Epithelial Systems. [Abstract]2025 Dec 23:e08648. PMID: 41431893 -
Adv Sci (Weinh)
CDK4/6 Inhibitors Impede Chemoresistance and Inhibit Tumor Growth of Small Cell Lung Cancer. [Abstract]2024 Aug 13:e2400666. PMID: 39136283
Palbociclib monohydrochloride 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.
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J Clin Invest
Dual targeting CDK4/6 and CDK7 augments tumor response and anti-tumor immunity in breast cancer models. [Abstract]2025 Aug 12:e188839. PMID: 40794455 -
Nucleic Acids Res
Rapid photo-crosslinking in living cells reveals protein-nucleic acid dynamics on a timescale of minutes. [Abstract]2026 Apr 13;54(7):gkag339. PMID: 42011781 -
Nucleic Acids Res
PARP1 and PARP2 are dispensable for DNA repair by microhomology-mediated end-joining at double-ended DSBs. [Abstract]2026 Jan 5;54(1):gkaf1437. PMID: 41495903 -
J Exp Clin Cancer Res
Integrated genomic analyses in PDX model reveal a cyclin-dependent kinase inhibitor Palbociclib as a novel candidate drug for nasopharyngeal carcinoma. [Abstract]2018 Sep 20;37(1):233. PMID: 30236142
Palbociclib monohydrochloride 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.
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Sci Adv
Somatic CRISPR tumorigenesis and multiomic analysis reveal a pentose phosphate pathway disruption vulnerability in MPNSTs. [Abstract]2025 Aug 15;11(33):eadu2906. PMID: 40802750 -
Mol Ther
2026 Mar 24:S1525-0016(26)00210-8. PMID: 41883164 -
Environ Sci Technol
Azocyclotin Binds CDK4 to Disrupt DNA Methylation in Zebrafish Epigenetic Transgenerational Inheritance. [Abstract]2025 Dec 23;59(50):27130-27142. PMID: 41359812 -
EBioMedicine
Enhancer demethylation-regulated gene score identified molecular subtypes, inspiring immunotherapy or CDK4/6 inhibitor therapy in oesophageal squamous cell carcinoma. [Abstract]2024 Jul:105:105177. PMID: 38924839 -
EBioMedicine
MYC status as a determinant of synergistic response to Olaparib and Palbociclib in ovarian cancer. [Abstract]2019 May:43:225-237. PMID: 30898650
Palbociclib monohydrochloride 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.
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EBioMedicine
Potent anti-tumor efficacy of palbociclib in treatment-naïve H3.3K27M-mutant diffuse intrinsic pontine glioma. [Abstract]2019 May:43:171-179. PMID: 31060906 -
MedComm (2020)
In vivo visualization of fluorescence reflecting CDK4 activity in a breast cancer mouse model. [Abstract]2022 Jun 10;3(3):e136. PMID: 35711853 -
Cell Rep Med
CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]2025 Dec 29:102526. PMID: 41468895 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Clin Cancer Res
ESR1 Y537S and D538G mutations drive resistance to CDK4/6 inhibitors in estrogen receptor-positive breast cancer. [Abstract]2025 May 1;31(9):1667-1675. PMID: 39992682 -
Clin Cancer Res
CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]2024 Sep 13;30(18):4179-4189. PMID: 39052240 -
Clin Cancer Res
Radiotherapy Delivered before CDK4/6 Inhibitors Mediates Superior Therapeutic Effects in ER+ Breast Cancer. [Abstract]2021 Apr 1;27(7):1855-1863. PMID: 33495311
Palbociclib monohydrochloride 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.
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Cancer Lett
A NIR-Ⅱ fluorescent probe for real-time visualization and early assessment of responses to CDK4/6 inhibitors in breast cancer. [Abstract]2026 May 28:646:218429. PMID: 41825845 -
Cancer Lett
PI3K inhibitor idelalisib enhances the anti-tumor effects of CDK4/6 inhibitor palbociclib via PLK1 in B-cell lymphoma. [Abstract]2024 May 28:216996. PMID: 38815797 -
Int J Biol Sci
Transcription Factor E2F4 Promote Proliferation, Migration, and Invasion of Gastric Cancer Cells by transcriptionally activating DSCC1. [Abstract]2024 Sep 16;20(12):4978-4998. PMID: 39309429 -
Int J Biol Sci
2021 Jan 31;17(3):728-741. PMID: 33767584 -
Int J Biol Sci
Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. [Abstract]2019 Jan 1;15(3):522-532. PMID: 30745839 -
Acta Biomater
2022 Sep 15:150:211-220. PMID: 35921992 -
Cell Death Dis
The RBPJ/DAPK3/UBE3A signaling axis induces PBRM1 degradation to modulate the sensitivity of renal cell carcinoma to CDK4/6 inhibitors. [Abstract]2022 Apr 2;13(4):295. PMID: 35368029 -
Cell Death Dis
c-myc regulates the sensitivity of breast cancer cells to palbociclib via c-myc/miR-29b-3p/CDK6 axis. [Abstract]2020 Sep 15;11(9):760. PMID: 32934206 -
Cell Death Dis
Pan-cancer analysis reveals synergistic effects of CDK4/6i and PARPi combination treatment in RB-proficient and RB-deficient breast cancer cells. [Abstract]2020 Apr 6;11(4):219. PMID: 32249776 -
Proc Natl Acad Sci U S A
2026 Feb 10;123(6):e2524246123. PMID: 41628322 -
Dev Cell
2023 Oct 9;58(19):1967-1982.e8. PMID: 37734383
Palbociclib monohydrochloride 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 monohydrochloride 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
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EMBO Mol Med
Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML. [Abstract]2025 Aug 29. PMID: 40883610 -
EMBO J
2024 Nov;43(22):5381-5420. PMID: 39327527 -
EMBO J
2024 Oct;43(19):4406-4436. PMID: 39160273 -
Phytomedicine
Hernandezine acts as a CDK4 suppressor inhibiting tumor growth by the CDK4/PKM2/NRF2 axis in colon cancer. [Abstract]2024 May 28:131:155775. PMID: 38838401 -
EMBO J
RNA sensing via the RIG-I-like receptor LGP2 is essential for the induction of a type I IFN response in ADAR1 deficiency. [Abstract]2022 Mar 15;41(6):e109760. PMID: 35156720 -
EMBO J
2021 Jun 1;40(11):e99692. PMID: 33856059 -
NPJ Precis Oncol
IL-6 predicts CDK4/6 inhibitor resistance, identifying STAT3 as a target in HR + /HER2-negative metastatic breast cancer. [Abstract]2025 Jul 25;9(1):260. PMID: 40715551 -
NPJ Precis Oncol
Acetylation of ELF5 suppresses breast cancer progression by promoting its degradation and targeting CCND1. [Abstract]2021 Mar 19;5(1):20. PMID: 33742100 -
Neoplasia
The antitumor activity of osimertinib plus palbociclib in non-small cell lung cancer patient-derived xenograft (PDX)/2D/3D culture models harboring EGFR amplification and CDKN2A/2B homozygous deletions. [Abstract]2024 Aug 14:57:101039. PMID: 39146623 -
Cell Syst
A Multi-center Study on the Reproducibility of Drug-Response Assays in Mammalian Cell Lines. [Abstract]2019 Jul 24;9(1):35-48.e5. PMID: 31302153 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Neoplasia
Combined Inhibition of ATR and WEE1 as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer. [Abstract]2018 Mar 28;20(5):478-488. PMID: 29605721 -
NPJ Breast Cancer
JAK/STAT1-interferon-ISGylation networks in breast cancer resistance to inhibitors of FOXM1 and CDK4/6. [Abstract]2026 Feb 12. PMID: 41680190 -
NPJ Breast Cancer
CDK2 inhibition enhances CDK4/6 inhibitor antitumor activity in comprehensive breast cancer PDX model screen. [Abstract]2025 Dec 3;11(1):135. PMID: 41339342 -
NPJ Breast Cancer
Discovery of a novel small molecule degrader of wild type and mutant estrogen receptors using DNA encoded libraries. [Abstract]2025 Nov 12;11(1):125. PMID: 41224743 -
NPJ Breast Cancer
MCM3 upregulation confers endocrine resistance in breast cancer and is a predictive marker of diminished tamoxifen benefit. [Abstract]2021 Jan 4;7(1):2. PMID: 33398005 -
Biomed Pharmacother
A brain-penetrant CDK4/6 inhibitor - AU3-14 shows robust anti-tumor efficacy against glioblastoma. [Abstract]2025 Aug:189:118340. PMID: 40651458 -
JHEP Rep
Loss of Cdkn1a protects against MASLD alone or with alcohol intake by preserving lipid homeostasis. [Abstract]2024 Oct 5;7(1):101230. PMID: 39659733 -
J Transl Med
Cellular senescence in the response of HR+ breast cancer to radiotherapy and CDK4/6 inhibitors. [Abstract]2023 Feb 10;21(1):110. PMID: 36765430 -
J Transl Med
2019 Aug 20;17(1):276. PMID: 31429774 -
Cell Mol Gastroenterol Hepatol
Additive Effect of CD73 Inhibitor in Colorectal Cancer Treatment With CDK4/6 Inhibitor Through Regulation of PD-L1. [Abstract]2022;14(4):769-788. PMID: 35843546 -
Oncogene
RB loss determines selective resistance and novel vulnerabilities in ER-positive breast cancer models. [Abstract]2022 Jul;41(27):3524-3538. PMID: 35676324 -
Cell Chem Biol
CDK2 heterobifunctional degraders co-degrade CDK2 and cyclin E resulting in efficacy in CCNE1-amplified and overexpressed cancers. [Abstract]2025 Apr 17;32(4):556-569.e24. PMID: 40250405 -
Cell Chem Biol
Multiomics Profiling Establishes the Polypharmacology of FDA-Approved CDK4/6 Inhibitors and the Potential for Differential Clinical Activity. [Abstract]2019 Aug 15;26(8):1067-1080.e8. PMID: 31178407 -
Cell Chem Biol
2018 Feb 15;25(2):135-142.e5. PMID: 29276047 -
Aging Cell
2022 Apr;21(4):e13580. PMID: 35266275 -
Eur J Cancer
Palbociclib enhances radiosensitivity of hepatocellular carcinoma and cholangiocarcinoma via inhibiting ataxia telangiectasia-mutated kinase-mediated DNA damage response. [Abstract]2018 Oct:102:10-22. PMID: 30103095
Palbociclib monohydrochloride 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.
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Cell Death Discov
CDK4/6 inhibition initiates cell cycle arrest by nuclear translocation of RB and induces a multistep molecular response. [Abstract]2024 Oct 26;10(1):453. PMID: 39461947 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Cell Rep
2023 Mar 30;42(4):112314. PMID: 37000627 -
Cell Rep
POLθ processes ssDNA gaps and promotes replication fork progression in BRCA1-deficient cells. [Abstract]2022 Nov 29;41(9):111716. PMID: 36400033 -
Cell Rep
S-palmitoylation of PCSK9 induces sorafenib resistance in liver cancer by activating the PI3K/AKT pathway. [Abstract]2022 Aug 16;40(7):111194. PMID: 35977495 -
Cell Rep
CDK/cyclin dependencies define extreme cancer cell-cycle heterogeneity and collateral vulnerabilities. [Abstract]2022 Mar 1;38(9):110448. PMID: 35235778 -
Cell Rep
Disentangling Pro-mitotic Signaling during Cell Cycle Progression using Time-Resolved Single-Cell Imaging. [Abstract]2020 Apr 14;31(2):107514. PMID: 32294432 -
Cell Rep
MicroRNA-Mediated Suppression of the TGF-β Pathway Confers Transmissible and Reversible CDK4/6 Inhibitor Resistance. [Abstract]2019 Mar 5;26(10):2667-2680.e7. PMID: 30840889 -
Br J Cancer
Transiently hypoxic tumour cell turnover and radiation sensitivity in human tumour xenografts. [Abstract]2022 Jun;126(11):1616-1626. PMID: 35031765 -
J Med Chem
Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase-1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation. [Abstract]2021 Nov 11;64(21):15702-15715. PMID: 34670362 -
J Med Chem
3 H-Pyrazolo[4,3- f]quinoline-Based Kinase Inhibitors Inhibit the Proliferation of Acute Myeloid Leukemia Cells In Vivo. [Abstract]2021 Aug 12;64(15):10981-10996. PMID: 34288692 -
Br J Cancer
2021 Jan;124(1):191-206. PMID: 33257837 -
Anal Chem
Minimally Invasive Single-Cell Metabolomics Analysis to Unveil Different Trajectories of Individual Cells in Ferroptosis. [Abstract]2026 Mar 24;98(11):8133-8142. PMID: 41814887 -
EMBO Rep
2022 Jun 7;23(6):e53932. PMID: 35403787 -
Ecotoxicol Environ Saf
PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]2025 Nov 15:307:119433. PMID: 41273832 -
Mol Ther Nucleic Acids
2023 Mar 21:32:302-317. PMID: 37096164 -
JCI Insight
2021 Apr 8;6(7):e139497. PMID: 33830080 -
Ecotoxicol Environ Saf
2020 Dec 1;205:111146. PMID: 32827965 -
Cancer Cell Int
2024 Dec 27;24(1):433. PMID: 39731167 -
Int J Mol Med
2025 Nov;56(5):167. PMID: 40808344 -
Breast Cancer Res
Lasofoxifene as a potential treatment for aromatase inhibitor-resistant ER-positive breast cancer. [Abstract]2024 Jun 7;26(1):95. PMID: 38849889 -
Cell Prolif
PFKFB4 facilitates palbociclib resistance in oestrogen receptor-positive breast cancer by enhancing stemness. [Abstract]2023 Jan;56(1):e13337. PMID: 36127291 -
Biochem Pharmacol
Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. [Abstract]2017 Jan 15:124:29-42. PMID: 27816545 -
Mol Cancer Ther
Harnessing senolytics and PARP inhibition to expand the antitumor activity of CDK4/6 inhibitors in prostate cancer. [Abstract]2025 Jul 2. PMID: 40601842 -
Inflamm Res
Cuproptosis-related gene CDKN2A as a molecular target for IPF diagnosis and therapeutics. [Abstract]2023 Jun;72(6):1147-1160. PMID: 37166466 -
Mar Drugs
A Marine Alkaloid, Ascomylactam A, Suppresses Lung Tumorigenesis via Inducing Cell Cycle G1/S Arrest through ROS/Akt/Rb Pathway. [Abstract]2020 Sep 27;18(10):494. PMID: 32992455 -
Liver Int
Epigenetic Regulation of MicroRNA Expression by Hepatitis B Virus Pre-S2 Mutant Promotes Hepatocellular Carcinoma Tumorigenesis. [Abstract]2026 Apr;46(4):e70582. PMID: 41797438 -
Cells
Characterization of a Preclinical In Vitro Model Derived from a SMARCA4-Mutated Sinonasal Teratocarcinosarcoma. [Abstract]2023 Dec 30;13(1):81. PMID: 38201285 -
J Pathol
Novel prognostication biomarker adipophilin reveals a metabolic shift in uveal melanoma and new therapeutic opportunities. [Abstract]2023 Jun;260(2):203-221. PMID: 36825655 -
Commun Biol
RBAP48 facilitates the oral squamous cell carcinoma process in an androgen receptor-dependent and independent manners. [Abstract]2025 May 30;8(1):829. PMID: 40442479 -
Life Sci
2023 Jun 1:322:121652. PMID: 37011871
Palbociclib monohydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121652. [Abstract]
Palbociclib (1 µM; 48 h) decreases the expression of PPARγ in SVFs.
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Int J Mol Sci
MYCN Amplification, along with Wild-Type RB1 Expression, Enhances CDK4/6 Inhibitors' Efficacy in Neuroblastoma Cells. [Abstract]2023 Mar 12;24(6):5408. PMID: 36982482 -
Int J Mol Sci
Therapeutic Potential for Regulation of the Nuclear Factor Kappa-B Transcription Factor p65 to Prevent Cellular Senescence and Activation of Pro-Inflammatory in Mesenchymal Stem Cells. [Abstract]2021 Mar 25;22(7):3367. PMID: 33805981 -
Int J Mol Sci
Cisplatin Synergistically Enhances Antitumor Potency of Conditionally Replicating Adenovirus via p53 Dependent or Independent Pathways in Human Lung Carcinoma. [Abstract]2019 Mar 5;20(5). pii: E1125. PMID: 30841620 -
Biomolecules
Targeting Cellular Senescence to Enhance Human Endometrial Stromal Cell Decidualization and Inhibit Their Migration. [Abstract]2025 Jun 16;15(6):873. PMID: 40563513 -
Mol Cancer Res
Dual Inhibition of CDK4 and CDK2 via Targeting p27 Tyrosine Phosphorylation Induces a Potent and Durable Response in Breast Cancer Cells. [Abstract]2018 Mar;16(3):361-377. PMID: 29330290 -
Molecules
2023 May 27;28(11):4380. PMID: 37298855 -
Mol Oncol
Dinaciclib synergizes with BH3 mimetics targeting BCL-2 and BCL-XL in multiple myeloma cell lines partially-dependent on MCL-1 and in plasma cells from patients. [Abstract]2023 Dec;17(12):2507-2525. PMID: 37704591 -
Mol Oncol
Palbociclib induces activation of AMPK and inhibits hepatocellular carcinoma in a CDK4/6-independent manner. [Abstract]2017 Aug;11(8):1035-1049. PMID: 28453226
Palbociclib monohydrochloride 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 monohydrochloride 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 monohydrochloride 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.
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Cancers (Basel)
Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]2024 Aug 7;16(16):2785. PMID: 39199558 -
Cancers (Basel)
Stromal Senescence following Treatment with the CDK4/6 Inhibitor Palbociclib Alters the Lung Metastatic Niche and Increases Metastasis of Drug-Resistant Mammary Cancer Cells. [Abstract]2023 Mar 22;15(6):1908. PMID: 36980794 -
Cancers (Basel)
Musashi1 Contribution to Glioblastoma Development via Regulation of a Network of DNA Replication, Cell Cycle and Division Genes. [Abstract]2021 Mar 24;13(7):1494. PMID: 33804958 -
Cancers
Targeting Pharmacokinetic Drug Resistance in Acute Myeloid Leukemia Cells with CDK4/6 Inhibitors. [Abstract]2020 Jun 16;12(6):1596. PMID: 32560251 -
Front Cell Dev Biol
FBXO2 Promotes Proliferation of Endometrial Cancer by Ubiquitin-Mediated Degradation of FBN1 in the Regulation of the Cell Cycle and the Autophagy Pathway. [Abstract]2020 Aug 31;8:843. PMID: 32984335 -
J Cell Mol Med
Bortezomib suppresses self-renewal and leukemogenesis of leukemia stem cell by NF-ĸB-dependent inhibition of CDK6 in MLL-rearranged myeloid leukemia. [Abstract]2021 Mar;25(6):3124-3135. PMID: 33599085 -
Transl Oncol
TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]2025 Jan 3:52:102264. PMID: 39756156 -
iScience
Multiomic characterization and drug testing establish circulating tumor cells as an ex vivo tool for personalized medicine. [Abstract]2022 Sep 6;25(10):105081. PMID: 36204272 -
J Cell Physiol
2025 Nov;240(11):e70113. PMID: 41287970 -
J Biol Chem
2026 Jun;302(6):111461. PMID: 41999888 -
Sci Rep
Ganoderma lucidum spore oil with Ganoderma lucidum and Ganoderma sinense extracts (G2SO) shows antitumor and Immunomodulatory effects in mice. [Abstract]2026 Jan 5;16(1):4751. PMID: 41491024 -
Sci Rep
Hybrid framework for lesion-aware, clinically coherent chest X-ray report generation using contrastive learning and large language models. [Abstract]2026 Jan 5;16(1):4645. PMID: 41492086 -
Sci Rep
Dual-drug codelivery gelatin-based hydrogel of ARV-471 and Palbociclib enhances synergistic effect in breast cancer treatment. [Abstract]2025 Nov 29. PMID: 41318792 -
Sci Rep
Steroid hormone receptors, exome sequencing and treatment responsiveness of breast cancer patient-derived xenografts originated in a South American country. [Abstract]2025 Jan 18;15(1):2415. PMID: 39827242 -
J Biol Chem
Targeting the mitotic kinase NEK2 enhances CDK4/6 inhibitor efficacy by potentiating genome instability. [Abstract]2025 Jan 16:108196. PMID: 39826695 -
J Biol Chem
Downregulation of the splicing regulator NSRP1 confers resistance to CDK4/6 inhibitors via activation of interferon signaling in breast cancer. [Abstract]2024 Dec 10:108070. PMID: 39667501 -
Sci Rep
Selective but not pan-CDK inhibition abrogates 5-FU-driven tissue factor upregulation in colon cancer. [Abstract]2024 May 8;14(1):10582. PMID: 38719932 -
J Biol Chem
Cyclin D1 extensively reprograms metabolism to support biosynthetic pathways in hepatocytes. [Abstract]2023 Dec;299(12):105407. PMID: 38152849 -
J Biol Chem
The adapter protein FADD provides an alternate pathway for entry into the cell cycle by regulating APC/C-Cdh1 E3 ubiquitin ligase activity. [Abstract]2023 Jun;299(6):104786. PMID: 37146968 -
Sci Rep
RNA disruption is a widespread phenomenon associated with stress-induced cell death in tumour cells. [Abstract]2023 Jan 31;13(1):1711. PMID: 36720913 -
Sci Rep
2021 Mar 8;11(1):5374. PMID: 33686114 -
J Virol
2023 Jun 29;97(6):e0037023. PMID: 37219458 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Cell Signal
2025 Jul:131:111709. PMID: 40037423 -
Biochim Biophys Acta
Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81. [Abstract]2017 Nov 20;1865(2):354-363. PMID: 29157894
Palbociclib monohydrochloride 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.
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Development
2023 May 1;150(9):dev200903. PMID: 37017267 -
J Bone Oncol
Identification of GPC3 mutation and upregulation in a multidrug resistant osteosarcoma and its spheroids as therapeutic target. [Abstract]2021 Sep 20:30:100391. PMID: 34611509 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Future Med Chem
2019 Feb;11(3):165-177. PMID: 30556417 -
Endocrinology
TRβ Agonism Induces Tumor Suppression and Enhances Drug Efficacy in Anaplastic Thyroid Cancer in Female Mice. [Abstract]2023 Aug 28;164(10):bqad135. PMID: 37702560 -
Front Oncol
CDK6 Immunophenotype Implicates Potential Therapeutic Application of CDK4/6 Inhibitors in Urothelial Carcinoma. [Abstract]2022 Apr 8;12:819003. PMID: 35463324 -
Discov Oncol
2025 May 19;16(1):814. PMID: 40388071 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
The role of palbociclib on the alterations in CDKN2, CCNE1, E2F3, MDM2 expressions as target genes of miR-141. [Abstract]2024 Aug 8;19(8):e0306545. PMID: 39116089 -
PLoS One
Quercetin inhibits the epithelial-mesenchymal transition and reverses CDK4/6 inhibitor resistance in breast cancer by regulating circHIAT1/miR-19a-3p/CADM2 axis. [Abstract]2024 Jul 11;19(7):e0305612. PMID: 38990915 -
Cell Biochem Biophys
Mechanistic Regulation of Epidermal Growth Factor and Hormonal Receptors by Kinase Inhibitors and Organofluorines in Breast Cancer Therapy. [Abstract]2025 Mar;83(1):1113-1137. PMID: 39316263 -
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Biochem Biophys Res Commun
Polyphyllin I enhances the anti-tumor efficacy of Palbociclib by reversing M2 macrophage polarization in lung cancer. [Abstract]2025 Jun 18:777:152228. PMID: 40578288 -
Biochem Biophys Res Commun
Glyoxalase 1 inhibitor BBGC suppresses the progression of chronic lymphocytic leukemia and promotes the efficacy of Palbociclib. [Abstract]2023 Apr 2:650:96-102. PMID: 36774689 -
Leuk Res
Targeting cyclin-dependent kinases 4/6 inhibits survival of megakaryoblasts in acute megakaryoblastic leukaemia. [Abstract]2022 Sep:120:106920. PMID: 35872339 -
Am J Transl Res
2019 Sep 15;11(9):6055-6065. PMID: 31632573 -
bioRxiv
Disrupted Mitochondrial Copper Homeostasis Promotes Ferroptotic Stress, Senescence and MASLD Progression. [Abstract]2026 Jun 17:2026.06.15.731916. PMID: 42367918 -
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bioRxiv
Distinct p21 dynamics drive alternative routes to whole-genome duplication through a common CDK4/6-dependent polyploid G0 state. [Abstract]2026 Jan 15:2026.01.15.699545. PMID: 41648389 -
bioRxiv
53BP1 condensates function as bioreactors for NHEJ directed DNA repair and insulators to determine pathway choice. [Abstract]2025 Dec 23:2025.12.19.695596. PMID: 41509350 -
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bioRxiv
2025 Nov 3:2025.11.02.685764. PMID: 41279360 -
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bioRxiv
Mitotic bypass and endocycling promote cancer cell survival after genotoxic chemotherapy. [Abstract]2025 Nov 4:2025.11.03.686258. PMID: 41278999 -
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bioRxiv
2024 Dec 5:2024.12.05.627000. PMID: 39677682 -
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bioRxiv
Therapeutic benefits of maintaining CDK4/6 inhibitors and incorporating CDK2 inhibitors beyond progression in breast cancer. [Abstract]2024 Nov 15:2024.11.11.623139. PMID: 39605351
Palbociclib monohydrochloride 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).
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
bioRxiv
2024 Nov 4:2024.10.08.617155. PMID: 39415993 -
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bioRxiv
Nanoparticle delivery of innate immune agonists combines with senescence-inducing agents to mediate T cell control of pancreatic cancer. [Abstract]2023 Sep 18:2023.09.18.558307. PMID: 37790484 -
bioRxiv
CDK6-mediated endothelial cell cycle acceleration drives arteriovenous malformations in hereditary hemorrhagic telangiectasia. [Abstract]2023 Sep 16:2023.09.15.554413. PMID: 37745444 -
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J Oncol
Palbociclib Enhances Migration and Invasion of Cancer Cells via Senescence-Associated Secretory Phenotype-Related CCL5 in Non-Small-Cell Lung Cancer. [Abstract]2022 Sep 27:2022:2260625. PMID: 37181790 -
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Solvent & Solubility
DMSO : 4.63 mg/mL (9.57 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (2.07 mM; ultrasonic and warming and heat to 60°C)
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* 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.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 0.54 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.4 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 0.54 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.4 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: Lactic acid buffer (50 mM, pH 4.0)
Solubility: 4.17 mg/mL (8.62 mM); Clear solution; Need ultrasonic
Add each solvent one by one: 0.5% HPMC/1% Tween-80 in Saline water
Solubility: 49.5 mg/mL (102.27 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Portuguese - PT (623 KB)
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Handling Instructions (2659 KB)
References
[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38. [Content Brief]
[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [Content Brief]
[3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. [Content Brief]
[4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. [Content Brief]
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.0662 mL | 10.3308 mL | 20.6616 mL | 51.6540 mL |
| DMSO | 5 mM | 0.4132 mL | 2.0662 mL | 4.1323 mL | 10.3308 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.