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Product Details

Palbociclib | CDK4/CDK6 inhibitor

Palbociclib (571190-30-2) is a potent and selective inhibitor of Cdk4, IC50 = 11 nM and Cdk6, IC50 = 16 nM.1 Inhibits phosphorylation of Rb protein and cell cycle progression through G1 in primary 5T33MM cells and sensitized these cells to killing by a proteasome inhibitor (bortezomib) in mouse models.2 Induces autophagy and senescence in AGS gastric cancer cells. Clinically useful breast cancer agent.4 Cell cycle inhibitors boost tumor immunogenicity.5   Palbociclib is able to regulate the PRMT5-MDM4 axis leading to decreased MDM4 protein expression and subsequent p53 activation via CDK4 inhibition.6

References/Citations

1) El-Rayes et al. (2004), Cyclooxygenase-2-dependent and –independent effects of celecoxib in pancreatic cancer cell lines; Mol. Cancer Ther., 3 1427
2) Menu et al. (2008), A novel therapeutic combination using PD 0332991 and bortezomib: study in 5T33MM myeloma model; Cancer Res., 68 5519
3) Valenzuela et al. (2017), Palbociclib-induced autophagy and senescence in gastric cancer cells; Exp. Cell Res., 360 390
4) Palanisamy et al. (2016), Palbociclib: A new hope in the treatment of breast cancer; J. Cancer Res. Ther., 12 1220
5) Goel et al. (2017), CDK4/6 inhibition triggers anti-tumour immunity; Nature 548 471
6)6) AbuHammad et al. (2019), Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma; Proc. Natl. Acad. Sci. USA 116 179909

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Focus Biomolecules cell signaling supplier, chemical structure of Palbociclib | CDK4/CDK6 inhibitor | CAS 571190-30-2

Catalog#  10-4760-0005

$50.00
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CAS:
571190-30-2
Catalog Number:
10-4760
Activity:
CDK4/CDK6 inhibitor
Chemical Name:
6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-piperazin-1-yl)pyridine-2-yl]amino]-8H-pyrido[2,3-d]pyrimidin-7-one
Alternate Names:
PD-332991
Molecular Weight:
447.53
Molecular Formula:
C24H29N7O2
Solubility:
Soluble in DMSO (up to 2 mg/ml with warming)
Physical Properties:
Yellow solid
Purity:
99% by HPLC/TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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