PD 0332991 HCl Inhibitor CAS No. 827022-32-2

Cat. No.	Name	Size	Price
KI0219	PD 0332991 HCl	5 mg	$176
	PD 0332991 HCl	10 mg	$272
	PD 0332991 HCl	50 mg	$912

Chemical Characteristic

Product Name	PD 0332991 HCl
CAS No.	827022-32-2
Molecular Weight	483.99
Formula	C₂₄H₂₉N₇O₂.HCl
Chemical Name	6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
Smiles	c1(nc2c(cn1)c(c(c(=O)n2C1CCCC1)C(=O)C)C)Nc1ccc(cn1)N1CCNCC1 Cl
Chemical Structure

Biological activities

PD 0332991 specifically inhibits cyclin-dependent kinase 4 (Cdk4)/cyclin D1 and (cyclin-dependent kinase 6) Cdk6/cyclin D2 with IC50 values of 11 and 16 nM, respectively. The IC50 values of PD 0332991 for reduction of retinoblastoma (Rb) phosphorylation at Ser⁷⁸⁰ and Ser⁷⁹⁵ are 66 and 63 nM in MDA-MB-435 breast carcinoma cells, respectively. Similar effects of PD 0332991 on both Ser⁷⁸⁰ and Ser⁷⁹⁵ phosphorylation are obtained in the Colo-205 colon carcinoma. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 40 to 170 nM. However, PD 0332991 (3 µM) exhibits no antiproliferative activity in the MDA-MB-468 human breast carcinoma and the H2009 human non??mall cell lung carcinoma, both of which have deleted Rb. PD 0332991 (0.04-10 µM) causes a significant increase in the percentage of MDA-MB-453 breast carcinoma cells in G1.^[1] PD 0332991 (10-50 nM) essentially completely inhibits BrdU incorporation in 3 mantle cell lymphoma (MCL) cell lines (Jeko-1, Mino and SP-53). PD 0332991 (200 nM) profoundly inhibits cell cycle progression at the G0/G1 phase in MCL cell lines and markedly reduces the proliferative rate of highly purified MCL cells.^[2] PD 0332991 (1 µM) inhibits Cdk4/6-specific phosphorylation of Rb on serine^807/811 (pSRb) in primary 5T33MM cells ex vivo. In 5T33MM diseased mice, PD 0332991 treatment (150 mg/kg) leads to a significant increase in survival, to a mean of 35 days in the PD 0332991??reated mice compared with 25 days in vehicle-treated mice. Besides, pSRb is reduced in primary 5T33MM tumor cells of ex vivo treatment with PD 0332991 (1 µM) or bortezomib (3 nM) alone, and further reduced by PD 0332991 and bortezomib combined.^[3] In mice bearing Colo-205 colon carcinoma xenografts (p16 deleted), PD 0332991 (150 or 75 mg/kg) produces rapid tumor regressions and a corresponding tumor growth delay of about 50 days at 150 mg/kg dose. In the MDA-MB-435 breast carcinoma (p16 deleted) xenografts model, 150 mg/kg PD 0332991 causes a complete tumor stasis. Furthermore, in the ZR-75-1 breast and PC-3 prostate tumor models, 150 mg/kg PD 0332991 also induces responses nearing stasis (complete suppression of tumor growth).^[1]

References

[1] 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, 3(11): 1427-1438. [2] Marzec M, et al. Mantle cell lymphoma cells express predominantly cyclin D1a isoform and are highly sensitive to selective inhibition of CDK4 kinase activity. Blood. 2006, 108(5): 1744-1750. [3] Menu E, et al. A novel therapeutic combination using PD 0332991 and bortezomib: study in the 5T33MM myeloma model. Cancer Res. 2008, 68(14): 5519-5523.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com