Home Tools

Palbociclib

Catalog No. T1785 CAS 571190-30-2

Synonyms: PD 0332991

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Palbociclib, CAS 571190-30-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 48.00
10 mg	In stock	$ 68.00
50 mg	In stock	$ 89.00
100 mg	In stock	$ 97.00

Bulk Inquiry

Select Batch

Purity: 99.9%

Purity: 99.76%

Purity: 99.23%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.
Targets&IC50	CDK4:11 nM, CDK6:16 nM
In vitro	METHODS: Malignant rhabdomyosarcoma cells G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) were treated with Palbociclib (0-1 mM) for 24 h, and cell viability was assayed by WST. RESULTS: Palbociclib effectively inhibited AN, RY, G401 and NS cell lines in a concentration-dependent manner, with IC50s of 0.01 μM, 0.01 μM, 0.06 μM and 0.6 μM, respectively; on the contrary, the YM cell line was resistant to Palbociclib, with an IC50 >10 μM.[1] METHODS: Human breast cancer cells MDA-MB-453 were treated with Palbociclib (0.02-10 μmol/L) for 24 h, and the cell cycle was examined by Flow Cytometry. RESULTS: Palbociclib caused G1 phase block. [2]
In vivo	METHODS: To detect antitumor activity in vivo, Palbociclib (12.5-150 mg/kg, sodium lactate buffer (50 mmol/L, pH 4.0)) was administered orally to immunodeficient mice harboring the tumors Colo-205 or MDA-MB-435 once daily for fourteen days. RESULTS: Palbociclib showed significant anti-tumor efficacy in multiple human tumor xenograft models. In Colo-205 tumors, PD 0332991 administered for 14 days produced rapid tumor regression. [2] METHODS: To assay antitumor activity in vivo, Palbociclib (150 mg/kg, sodium lactate buffer (50 mM, pH = 4.0)) was administered once daily for two weeks by gavage to nu/nu BALB/c mice bearing esophageal squamous cell carcinoma (ESCC) tumors EC109 or KYSE150. RESULTS: Palbociclib effectively inhibited ESCC tumor growth and lung metastasis. [3]
Kinase Assay	CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792-928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and Palbociclib (0.001-0.1 μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25°C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4°C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.
Cell Research	Palbociclib (PD) is prepared in DMSO and stored (?80°C), and then diluted with appropriate media before use[1]. MRT cell lines, G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) cell lines are seeded in normal growth medium into 96-well cell plates. After 24 h, the culture medium is replaced with culture medium containing Palbociclib (0.05 or 1 μM) or DMSO. Cells are cultured and treated in triplicate. Cell proliferation is determined 8 days after the treatment by WST-8 assay using a Cell Counting Kit-8.

Synonyms	PD 0332991
Molecular Weight	447.53
Formula	C24H29N7O2
CAS No.	571190-30-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 1.3 mg/mL, Sonication is recommended.

References and Literature

1. Katsumi Y, et al. Sensitivity of malignant rhabdoid tumor cell lines to PD 0332991 is inversely correlated with p16 expression. Biochem Biophys Res Commun. 2011 Sep 16;413(1):62-8. 2. 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. 3. Chen L, et al. Dual cyclin-dependent kinase 4/6 inhibition by PD-0332991 induces apoptosis and senescence in oesophageal squamous cell carcinoma cells. Br J Pharmacol. 2017 Aug;174(15):2427-2443.

Citations

1. Jiang Z, Cheng L, Wu Z, et al. Transforming primary human hepatocytes into hepatocellular carcinoma with genetically defined factors. EMBO reports. 2022: e54275 2. Qin Z, Hu H, Sun W, et al. miR-224-5p Contained in Urinary Extracellular Vesicles Regulates PD-L1 Expression by Inhibiting Cyclin D1 in Renal Cell Carcinoma Cells. Cancers. 2021 Feb 4;13(4):618. doi: 10.3390/cancers13040618. 3. Liu Z, Zhao Y, Kong P, et al.Integrated multi-omics profiling yields a clinically relevant molecular classification for esophageal squamous cell carcinoma.Cancer Cell.2022 4. Wu M, Zhang X, Zhang W, et al.Paracrine secretion of IL8 by breast cancer stem cells promotes therapeutic resistance and metastasis of the bulk tumor cells.Cell Communication and Signaling.2023, 21(1): 1-17. 5. Hong J H, Yong C H, Heng H L, et al.Integrative multiomics enhancer activity profiling identifies therapeutic vulnerabilities in cholangiocarcinoma of different etiologies.Gut.2023

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library FDA-Approved Kinase Inhibitor Library EMA Approved Drug Library Kinase Inhibitor Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

SR-4835 CDK12-IN-2 KB-0742 dihydrochloride CDK9-IN-2 THZ1 2HCl Palbociclib Isethionate Trilaciclib Isoangustone A

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Palbociclib 571190-30-2 Cell Cycle/Checkpoint CDK PD 0332991 PD-0332991 estrogen receptor HER2 HCC inhibit Inhibitor Cyclin dependent kinase hepatocellular carcinoma cell cycle PD0332991 Breast cancer inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.