R&D Systems Inc. Tocris Bioscience Boston Biochem

PD 0332991 isethionate

Cat. No. 4786

PD 0332991 isethionate C24H29N7O2.C2H6O4S [827022-33-3]

Price and Availability

For PD 0332991 isethionate pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one isethionate salt

Biological Activity

Potent Cdk4/6 inhibitor (IC50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10 μM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
573.66
Formula:
C24H29N7O2.C2H6O4S
Solubility:
Soluble to 100 mM in water and to 10 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
827022-33-3

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

References

Fry et al (2004) Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol.Cancer Ther. 3 1427. PMID: 15542782.

Toogood et al (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 48 2388. PMID: 15801831.

Michaud et al (2010) Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res. 70 3228. PMID: 20354191.

If you know of a relevant citation for this product please let us know.

View Related Products by Target

Keywords: PD 0332991 isethionate, supplier, PD0332991, isethionate, cyclin, dependent, kinases, Cdk4, Cdk6, selective, potent, inhibitors, inhibits, antitumor, G1, cell, cycle, arrest, brain, penetrant

Quick Order

Find multiple products by catalog number

divider line

Cancer Research Product Guide

Cancer Research Guide

Highlights over 350 products for cancer research. Request a copy or view PDF today.

divider line

Kinases Product Listing

Kinases Product Listing

Highlights over 350 products for kinase research. Request a copy or view PDF today.

divider line

Kinase Inhibitor Toolbox

80 Kinase inhibitors
pre-dissolved in DMSO

Kinase Inhibitor Toolbox

Includes many of the latest kinase inhibitors to become commercially available. Covers a wide range of kinase targets including EGFR, MAPK and CDK.

divider line

Checkpoint Kinases & the DNA Damage Response

Written by Michelle D. Garrett and Ian Collins

Cell Cycle Kinases Poster

A summary of the response of the checkpoint kinase signaling network to DNA damage, including activation of DNA repair, cell-cycle arrest, senescence and apoptosis.

divider line

New Product Guide

NPG

Highlights 140 new products added in the first half of 2014. Request a copy or view PDF today.

divider line

New Products in this Area

ZLN 024 hydrochloride

Allosteric AMPK activator

Temsirolimus

mTOR inhibitor; antitumor

KN 93 phosphate

CaM kinase II inhibitor; water soluble version of KN 93 (Cat. No. 1278).

Bryostatin 3

Potent protein kinase C activator

GKA 50

Glucokinase activator

MRT 67307 dihydrochloride

Salt inducible kinase (SIK) inhibitor

LDN 209929 dihydrochloride

Potent and selective haspin kinase inhibitor

RKI 1447 dihydrochloride

Potent and selective ROCK inhibitor; antitumor

LIMKi 3

Potent LIM kinase inhibitor; antitumor

FRAX 486

Potent p21-activated kinase (PAK) inhibitor; brain penetrant and orally bioavailable

BIX 02189

Selective MEK5 and ERK5 inhibitor

TC Mps1 12

Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor; orally active

GSK 2606414

Potent and selective PERK inhibitor; orally bioavailable

AZ 20

Potent and selective ATR kinase inhibitor; antitumor

AZD 7762 hydrochloride

Potent and selective ATP-competitive inhibitor of Chk1 and Chk2

PHT 427

Dual Akt and PDK1 inhibitor; antitumor

Sign-up for new product e-alerts
divider line

Twitter Updates

Follow @Tocris on Twitter

Follow us on Twitter!

Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.