Palbociclib

Manufactured by Pfizer

Sourced in United States, Germany, Italy

Palbociclib is a cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. It functions by blocking the activity of CDK4 and CDK6, which are involved in cell cycle progression.

Automatically generated - may contain errors

Lab products found in correlation

Trametinib, by Selleck Chemicals (3 mentions) Pd0325901, by Pfizer (2 mentions) Bazedoxifene, by Pfizer (2 mentions) Pd0325901, by Selleck Chemicals (2 mentions) Fetal bovine serum (fbs), by Thermo Fisher Scientific (2 mentions) Everolimus, by Selleck Chemicals (1 mentions) Binimetinib, by Selleck Chemicals (1 mentions) Ulixertinib, by Selleck Chemicals (1 mentions) Erlotinib, by Selleck Chemicals (1 mentions) Ly2874455, by Selleck Chemicals (1 mentions) Mk 2206, by Selleck Chemicals (1 mentions) Celltiter glo, by Promega (1 mentions) Britton robinson buffer, by Merck Group (1 mentions) Methanol, by Merck Group (1 mentions) Urea, by Merck Group (1 mentions) Pd0332991, by Pfizer (1 mentions) Jagged 1 fc, by Abcam (1 mentions) Rpmi 1640 medium, by Merck Group (1 mentions) Hyclone, by Cytiva (1 mentions) Sabutoclax, by Selleck Chemicals (1 mentions)

36 protocols using palbociclib

Palbociclib Dosage and Administration

Check if the same lab product or an alternative is used in the 5 most similar protocols

Palbociclib was obtained from Pfizer Inc. Palbociclib powder was stored at room temperature and protected from light.
For in vitro experiments, a 2.5 mM stock of Palbociclib was prepared in DMSO and stored as single use aliquots at -80ºC.
For in vivo experiments, Palbociclib was dissolved in Sodium L-Lactate (Sigma-Aldrich; St. Louis, MO) buffer (50mM, pH 4.0). Cre:ER T+/-PTEN f/f mice were given a single daily dose of 100 mg/kg of Palbociclib by oral gavage, starting two weeks after tamoxifen injection. For Palbociclib acute treatment, Cre-ER T+/-PTEN fl/fl animals were treated for three consecutive days with 75, 100 or 150 mg/kg of the inhibitor. For survival experiments, mice received 5 doses per week until the moment of sacrifice. In each experiment, control animals were given vehicle following the same schemes.

Dosil M.A., Mirantes C., Eritja N., Felip I., Navaridas R., Gatius S., Santacana M., Colàs E., Moiola C., Schoenenberger J.A., Encinas M., Garí E., Matias-Guiu X, & Dolcet X. (2017). Palbociclib has antitumour effects on Pten-deficient endometrial neoplasias. The Journal of pathology, 242(2).

+ Open protocol

+ Expand

Culturing Breast Cancer Cell Lines

Check if the same lab product or an alternative is used in the 5 most similar protocols

MCF7 (ATCC HTB-22) and T47D (ATCC HTB-133) human breast cancer cells were obtained from ATCC and cultured in phenol red–free RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS, Euroclone), 2 mmol/L glutamine and 1 nmol/L 17β-estradiol (E2, Sigma). The corresponding LTED derivatives were maintained in a sterol-deprived medium in phenol red–free RPMI 1640 medium containing 10% dextran charcoal-stripped FBS (Hyclone) and 2 mmol/L glutamine (DCC medium). The palbociclib-resistant derivatives (PalboR) were cultured in in DCC medium in the presence of 1 µM palbociclib (Pfizer, Pfizer Italia, Latina, Italy). Cells were short tandem repeat tested, amplified, stocked, routinely subjected to mycoplasma testing and once thawed were kept in culture for a maximum of 20 passages.

El-Botty R., Morriset L., Montaudon E., Tariq Z., Schnitzler A., Bacci M., Lorito N., Sourd L., Huguet L., Dahmani A., Painsec P., Derrien H., Vacher S., Masliah-Planchon J., Raynal V., Baulande S., Larcher T., Vincent-Salomon A., Dutertre G., Cottu P., Gentric G., Mechta-Grigoriou F., Hutton S., Driouch K., Bièche I., Morandi A, & Marangoni E. (2023). Oxidative phosphorylation is a metabolic vulnerability of endocrine therapy and palbociclib resistant metastatic breast cancers. Nature Communications, 14, 4221.

+ Open protocol

+ Expand

KRAS-mutant NSCLC Cell Line Profiling

Check if the same lab product or an alternative is used in the 5 most similar protocols

KRAS-mutant NSCLC cell lines were authenticated and maintained in the recommended medium. Palbociclib (PD0332991) and PD0325901 were supplied by Pfizer. Trametinib, binimetinib, ulixertinib, everolimus, MK2206, erlotinib, LY2874455 and LMN-211904 were obtained from Selleckchem, and bFGF neutralizing antibody was obtained from Sigma. For depletion experiments, pLKO.1 shRNA constructs targeting CDK1, CDK2, CDK4, CDK6, cyclin D1, cyclin D3 and cyclin E (Harvard PlasmID Database) were expressed by lentiviral infection. Palbociclib-resistant cells H358-PR100, H358-PR250, H460-PR500 and H441-PR500 were isolated after the serial addition of increasing concentrations of Palbociclib to culture media. Resistance was confirmed by assessment of proliferation and cell cycle analysis in the presence of Palbociclib. Cell viability assays were performed using CellTiter-Glo (Promega) starting with 1 × 10³ cells in 96-well plates.

Haines E., Chen T., Kommajosyula N., Chen Z., Herter-Sprie G.S., Cornell L., Wong K.K, & Shapiro G.I. (2018). Palbociclib resistance confers dependence on an FGFR-MAP kinase-mTOR-driven pathway in KRAS-mutant non-small cell lung cancer. Oncotarget, 9(60), 31572-31589.

+ Open protocol

+ Expand

Cytotoxicity Evaluation of Palbociclib

Check if the same lab product or an alternative is used in the 5 most similar protocols

- Palbociclib was obtained from Pfizer, Freiburg, Germany.
- Urea, Britton-Robinson buffer, and methanol were purchased from Sigma Aldrich (St. Louis, MO, USA).
- HepG2 cell line was obtained from Nawah Scientific Company, Egypt.
- All materials and reagents were of analytical grade.
- Double distilled water was utilized throughout the work.

Magdy G., Belal F, & Elmansi H. (2023). Rapid microwave-assisted synthesis of nitrogen-doped carbon quantum dots as fluorescent nanosensors for the spectrofluorimetric determination of palbociclib: application for cellular imaging and selective probing in living cancer cells. RSC Advances, 13(7), 4156-4167.

+ Open protocol

+ Expand

Regulation of DUB3 by CDK Phosphorylation

Check if the same lab product or an alternative is used in the 5 most similar protocols

Example 11

It was tested whether other CDKs could directly phosphorylate DUB3. Bacterially-expressed GST-DUB3 WT and GST-DUB3 S41A fusion polypeptides were incubated with active CDK4, CDK6, CDK1 or CDK2 in the presence of [γ-³²P]ATP. As shown in FIG. 15A, CDK1 directly phosphorylated DUB3 in vitro. Cells were transfected with FLAG-DUB3 WT, and were treated with a pan CDK inhibitor (Roscovitine) or a selective inhibitor of CDK 4/6, PD0332991 (Palbociclib, Pfizer). CDK inhibition dramatically reduced the phosphorylation of DUB3 at Ser41 (FIG. 15B).

US10690673B2. Method of treating cancer metastasis by CDK 4/6 inhibitors (2020-06-23). Mayo Foundation for Medical Education and Research [US]. Inventors: Zhenkun Lou [US], Tongzheng Liu [US].

+ Open protocol

+ Expand

Palbociclib and Notch Pathway Modulation in Gastric Cancer

Check if the same lab product or an alternative is used in the 5 most similar protocols

The AGS and HGC-27 GC cell lines were obtained from the American Type Culture Collection. All cells were cultured in RPMI-1640 medium (Sigma-Aldrich; Merck KGaA) containing 10% fetal bovine serum (Gibco; Thermo Fisher Scientific, Inc.) and 1% penicillin/streptomycin (HyClone; Cytiva) and maintained at 37°C in a humidified incubator containing 5% CO₂. Palbociclib was purchased from Pfizer (PD0332991), dissolved in DMSO and added into the culture medium at the indicated concentration. Cells were exposed to drug treatment for 2 days at 37°C, unless otherwise indicated. Cells were randomly divided into seven groups: i) Control (0 µM Palbociclib); ii) 0.25 µM Palbociclib; iii) 0.5 µM Palbociclib; iv) 1 µM Palbociclib; v) 2 µM Palbociclib; vi) 4 µM Palbociclib and vii) 0.5 µM Palbociclib + 10 µM Jagged-1/FC. The activator of Notch pathway (Jagged-1/FC) was supplied by Abcam.

Bi H., Shang J., Zou X., Xu J, & Han Y. (2021). Palbociclib induces cell senescence and apoptosis of gastric cancer cells by inhibiting the Notch pathway. Oncology Letters, 22(2), 603.

+ Open protocol

+ Expand

Modeling Ph+ ALL in NOD/SCID-IL-2Rγ-null Mice

Check if the same lab product or an alternative is used in the 5 most similar protocols

Ph+ ALL cells (2×10⁶ cells/mouse) were injected intravenously in 6–8 weeks old NOD/SCID-IL-2Rγ-null mice (Jackson Laboratory). Doxycycline was administered at 2 g/L in the drinking water starting 7 days post injection. Peripheral blood leukemic cells were monitored by flow cytometry detection of GFP, human CD10 and/or CD19 (based on cell type specific expression). For immunoblot analysis, leukemic cells were purified from murine cells by FACS or with the EasySep™ Mouse/Human Chimera Isolation Kit (StemCell Technologies). Palbociclib (obtained by Pfizer) was dissolved at 15 mg/mL in 50 mM sodium lactate, pH = 4.0 and given by oral gavage for 10 consecutive days at 150 mg/kg. Sabutoclax (SelleckChem) was dissolved at 0.5 mg/mL in 10:10:80 Kolliphor-EL (Sigma-Aldrich)-ethanol-PBS and administered intraperitoneally every other day at 5 mg/kg for a total of five doses. Animal experiments were approved by Thomas Jefferson University IACUC under protocol number 00012.

De Dominici M., Porazzi P., Soliera A.R., Mariani S.A., Addya S., Fortina P., Peterson L.F., Spinelli O., Rambaldi A., Martinelli G., Ferrari A., Iacobucci I, & Calabretta B. (2017). Targeting CDK6 and BCL2 exploits the “MYB addiction” of Ph+ acute lymphoblastic leukemia. Cancer research, 78(4), 1097-1109.

+ Open protocol

+ Expand

Synergistic effects of cell-cycle inhibitors

Check if the same lab product or an alternative is used in the 5 most similar protocols

Palbociclib was obtained from Pfizer (New York City, NY, USA). Danusertib (PHA-739358), alisertib (MLN8237), tozasertib (VX-680), CCT137690, everolimus (RAD001), MK-2206 2HCl, and ipatasertib (GDC-0068) were purchased from Selleckchem (Houston, TX, USA). For dose–response curves and synergy matrixes, cells were plated in triplicates in 96-well plates. ATP content was measured using CellTiterGlo (Fitchburg, WI, USA) according to the manufacturer’s instructions. IC₅₀ determination was performed using GraphPad^®. The percentage deviation from Bliss independency model [44 (link)] was determined via the following formula: Exy = Ex + Ey − (ExEy). E represents the effect on viability of drugs x and y, expressed as a percentage of the maximum effect. Cell cycle profiles were obtained by staining cells with propidium iodide (50 μg/mL) in hypotonic lysis solution (0.1% (w/v) sodium citrate, 0.1% (v/v) Triton X-100, 100 μg/mL RNAse) and incubating at 37 °C for 30 min before measurement via FACS.

Uras I.Z., Maurer B., Nebenfuehr S., Zojer M., Valent P, & Sexl V. (2018). Therapeutic Vulnerabilities in FLT3-Mutant AML Unmasked by Palbociclib. International Journal of Molecular Sciences, 19(12), 3987.

+ Open protocol

+ Expand

Evaluating ESR1 Ligands and Inhibitors

Check if the same lab product or an alternative is used in the 5 most similar protocols

ESR1 ligands included 17β-estradiol (Sigma), ICI 182,780 (Tocris), and 4-hydroxytamoxifen (Sigma). Palbociclib, pipendoxifene and bazedoxifene were provided by Pfizer. (S)-3-(3-hydroxyphenyl)-4-methyl-2-(4-((S)-2-((R)-3-methylpyrrolidin-1-yl)propoxy)phenyl)-2H-chromen-6-ol (BPN1) and (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid (BPL2) were synthesized as described (14 , 15 ). Ligands were dissolved in ethanol or DMSO.

Wardell S.E., Ellis M.J., Alley H.M., Eisele K., VanArsdale T., Dann S.G., Arndt K.T., Primeau T., Griffin E., Shao J., Crowder R., Lai J.P., Norris J.D., McDonnell D.P, & Li S. (2015). Efficacy of SERD/SERM Hybrid-CDK4/6 inhibitor combinations in models of endocrine therapy resistant breast cancer. Clinical cancer research : an official journal of the American Association for Cancer Research, 21(22), 5121-5130.

+ Open protocol

+ Expand

Preparation of Trametinib and Palbociclib

Check if the same lab product or an alternative is used in the 5 most similar protocols

Trametinib was purchased from LC Laboratories (Woburn, MA). Palbociclib was obtained under a Material Transfer Agreement from Pfizer Global R & D. For cellular studies, drugs were dissolved in DMSO at a concentration of 10mM and stock solutions stored at −20°C.

Ziemke E.K., Dosch J.S., Maust J.D., Shettigar A., Sen A., Welling T.H., Hardiman K.M, & Sebolt-Leopold J.S. (2015). Sensitivity of KRAS-Mutant Colorectal Cancers to Combination Therapy that Co-Targets MEK and CDK4/6. Clinical cancer research : an official journal of the American Association for Cancer Research, 22(2), 405-414.

+ Open protocol

+ Expand

About PubCompare

Our mission is to provide scientists with the largest repository of trustworthy protocols and intelligent analytical tools, thereby offering them extensive information to design robust protocols aimed at minimizing the risk of failures.

We believe that the most crucial aspect is to grant scientists access to a wide range of reliable sources and new useful tools that surpass human capabilities.

However, we trust in allowing scientists to determine how to construct their own protocols based on this information, as they are the experts in their field.

Ready to get started?

Revolutionizing how scientists
search and build protocols!