Palbociclib

Synonyms: PD 0332991

Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!

Palbociclib Chemical Structure

Palbociclib Chemical Structure

CAS: 571190-30-2

Selleck's Palbociclib has been cited by 113 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

Choose Selective CDK Inhibitors

Biological Activity

Description Palbociclib (PD 0332991) is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) and Cdk6 with IC50 of 11 nM and 16 nM, respectively.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
Targets
Cdk4 [1]
(Cell-free assay)
Cdk6 [1]
(Cell-free assay)
11 nM 16 nM
In vitro
In vitro

Palbociclib, a CKD4/6 inhibitor, significantly reduces HR+/HER2+ tumor cell viability when combinates with tucatinib and fulvestrant.[2]

Cell Research Cell lines BT474 and MDA-MB-361 tumor cell lines
Concentrations 0-15 μM
Incubation Time 72 h
Method

Cell viability is measured by Cell Titer Glo assay after 72 hours of treatment with vehicle or drugs. For all experiments with fulvestrant, cells are grown in estrogen free conditions, and estradiol is added to a final concentration of 10-8 M prior to drug treatment. Palbociclib, fulvestrant, and tucatinib IC30 values are calculated for each cell line, and the IC30 concentrations are used for subsequent experiments.

In Vivo
In vivo

Palbociclib, a CKD4/6 inhibitor, shows superior efficacy in suppression of tumor growth in vivo when combinates with tucatinib and fulvestrant.[2]

Animal Research Animal Models NCG mice injected with MDA-MB-361 cells
Dosages 50mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05912933 Not yet recruiting Breast Cancer Pfizer March 1 2024 --
NCT05709158 Not yet recruiting Breast Cancer Pfizer March 1 2024 --
NCT05665361 Recruiting Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc) National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 12 2024 Phase 1|Phase 2
NCT06076772 Not yet recruiting Metastatic Breast Cancer Assiut University November 2023 --
NCT05655598 Recruiting Advanced Breast Cancer|Treatment-Refractory Solid Tumors|Retinoblastoma Deficiency|SCLC|Soft Tissue Sarcoma|Endometrial Cancer|Bladder Cancer Brown University September 12 2023 Phase 1

Chemical lnformation & Solubility

Molecular Weight 447.53 Formula

C24H29N7O2

CAS No. 571190-30-2 SDF --
Smiles CC(=O)C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N(C5CCCC5)C1=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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