Palbociclib

Catalog No.S4482 Batch:S448201

Technical Data

Formula	C₂₄H₂₉N₇O₂
Molecular Weight	447.53	CAS No.	571190-30-2
Solubility (25°C)*	In vitro	5% TFA	5 mg/mL (11.17 mM)
		DMSO	Insoluble
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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

In vivo

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

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[2]}	Animal Models NCG mice injected with MDA-MB-361 cells Dosages 50mg/kg Administration o.g.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[2]}

Animal Models
NCG mice injected with MDA-MB-361 cells
Dosages
50mg/kg
Administration
o.g.

References

Selleck's Palbociclib has been cited by 117 publications

Chronic stress increases metastasis via neutrophil-mediated changes to the microenvironment [ Cancer Cell, 2024, S1535-6108(24)00037-0]	PubMed: 38402610
A renal clearable fluorogenic probe for in vivo β-galactosidase activity detection during aging and senolysis [ Nat Commun, 2024, 15(1):775]	PubMed: 38278798
Therapy-Induced Senescence Contributes to the Efficacy of Abemaciclib in Patients with Dedifferentiated Liposarcoma [ Clin Cancer Res, 2024, 30(4):703-718]	PubMed: 37695642
Intracellular calcium links milk stasis to lysosome-dependent cell death during early mammary gland involution [ Cell Mol Life Sci, 2024, 81(1):29]	PubMed: 38212474
DUB3 is a MAGEA3 deubiquitinase and a potential therapeutic target in hepatocellular carcinoma [ iScience, 2024, 27(3):109181]	PubMed: 38414853
Testing Adaptive Therapy Protocols Using Gemcitabine and Capecitabine in a Preclinical Model of Endocrine-Resistant Breast Cancer [ Cancers (Basel), 2024, 16(2)257]	PubMed: 38254748
IRF3 activates RB to authorize cGAS-STING-induced senescence and mitigate liver fibrosis [ Sci Adv, 2024, 10(9):eadj2102]	PubMed: 38416816
D-type cyclins regulate DNA mismatch repair in the G1 and S phases of the cell cycle, maintaining genome stability [ bioRxiv, 2024, 2024.01.12.575420]	PubMed: 38260436
p21 Prevents the Exhaustion of Cluster of Differentiation 4-Positive T Cells Within the Antitumor Immune Response Against Colorectal Cancer [ Gastroenterology, 2023, S0016-5085(23)05008-4]	PubMed: 37734420
Toxic PARP trapping upon cAMP-induced DNA damage reinstates the efficacy of endocrine therapy and CDK4/6 inhibitors in treatment-refractory ER+ breast cancer [ Nat Commun, 2023, 10.1038/s41467-023-42736-y]	PubMed: 37914699

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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