PD 0332991 isethionate
Cat. No. 4786
Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-[
Biological ActivityPotent 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 InformationSold for research purposes under agreement from Pfizer Inc.
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
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.
Keywords: PD 0332991 isethionate, supplier, PD0332991, isethionate, cyclin, dependent, kinases, Cdk4, Cdk6, selective, potent, inhibitors, inhibits, antitumor, G1, cell, cycle, arrest, brain, penetrant
Find multiple products by catalog number
New Products in this Area
Salt inducible kinase (SIK) inhibitorLDN 209929 dihydrochloride
Potent and selective haspin kinase inhibitorRKI 1447 dihydrochloride
Potent and selective ROCK inhibitor; antitumorLIMKi 3
Potent LIM kinase inhibitor; antitumorFRAX 486
Potent p21-activated kinase (PAK) inhibitor; brain penetrant and orally bioavailableBIX 02189
Selective MEK5 and ERK5 inhibitorTC Mps1 12
Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor; orally activeGSK 2606414
Potent and selective PERK inhibitor; orally bioavailableAZ 20
Potent and selective ATR kinase inhibitor; antitumorAZD 7762 hydrochloride
Potent and selective ATP-competitive inhibitor of Chk1 and Chk2PHT 427
Dual Akt and PDK1 inhibitor; antitumorML 786 dihydrochloride
Potent Raf kinase inhibitor; orally bioavailableSenexin A
Cyclin-dependent kinase 8 (cdk8) inhibitorXL 388
Potent and selective mTOR inhibitor; antitumorPS 1145 dihydrochloride
Selective IKK inhibitor; orally activeRSVA 405
AMPK activatorAtiprimod dihydrochloride
JAK2 inhibitorAIM 100
Potent and selective Ack1 inhibitorML 120B dihydrochloride
Novel IKK2-selective inhibitorML 202
Pyruvate kinase M2 activator
October 5 - 8, 2014