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PZ0199

Sigma-Aldrich

PD 0332991 isethionate

≥98% (HPLC), powder, cyclin dependent kinases (CDK4, CDK6) inhibitor

Synonyme(s) :

6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one 2-hydroxy-ethanesulfonic acid (1:1), Palbociclib isethionate

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About This Item

Formule empirique (notation de Hill):
C24H29N7O2 · C2H6O4S
Numéro CAS:
827022-33-3
Poids moléculaire :
573.66
Numéro MDL:
MFCD22666589
Code UNSPSC :
12352200
ID de substance PubChem :
329823771
Nomenclature NACRES :
NA.77

product name

PD 0332991 isethionate, ≥98% (HPLC)

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

H2O: 5 mg/mL, clear

Température de stockage

room temp

Chaîne SMILES 

OCCS(O)(=O)=O.CC(=O)C1=C(C)c2cnc(Nc3ccc(cn3)N4CCNCC4)nc2N(C5CCCC5)C1=O

InChI

1S/C24H29N7O2.C2H6O4S/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32;3-1-2-7(4,5)6/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29);3H,1-2H2,(H,4,5,6)

Clé InChI

LYYVFHRFIJKPOV-UHFFFAOYSA-N

Informations sur le gène

human ... CCND1(595) , CDK4(1019) , CDK6(1021)

Application

PD 0332991 isethionate has been used:
  • to incubate MCF10A cells to verify cyclin D1 inhibition of autophagy involved cyclin-dependent kinase activity
  • as a cyclin dependent kinase 4 (CDK4) inhibitor to study its anticonvulsive property in Drosophila
  • to mimic the inhibitory effect of 5α-dihydrotestosterone (DHT) on HPr-1AR cell cycle progression and growth

Actions biochimiques/physiologiques

PD 0332991 is a potent selective inhibitor of cyclin dependent kinases CDK4 and CDK6 with in vitro IC50 = 11 nM (CDK4) and 16 nM (CDK6). PD 0332991 induces G1 arrest in retinoblastoma (Rb)-positive tumor cells.
PD 0332991 might act as a chemsensitizer. It is useful in the treatment of breast cancer along with antioestrogens. PD 0332991 is also known to possess antitumor action.

Caractéristiques et avantages

This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Autres remarques

PD0332991 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PD0332991 probe summary on the Chemical Probes Portal website.

Pictogrammes

Skull and crossbones
GHS06

Mention d'avertissement

Danger

Mentions de danger

H301

Classification des risques

Acute Tox. 3 Oral

Code de la classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Kan Yaguchi et al.
Biochemical and biophysical research communications, 504(1), 231-237 (2018-09-09)
Near-haploidy is observed in certain cancer types, but ploidy-dependent alterations in gene regulation in the haploid state remain elusive. Here, by comparative transcriptome analysis between human isogenic haploid and diploid cell lines, we found lowering of cyclin D2 level in
Seizure suppression through manipulating splicing of a voltage-gated sodium channel
Lin WH, et al.
Brain, 138(4), 891-901 (2015)
Claudio A Valenzuela et al.
Experimental cell research, 360(2), 390-396 (2017-09-28)
Targeting cyclin D-CDK4/6 kinase complexes has recently been shown to increase the survival of breast cancer patients with estrogen receptor positive breast tumors. Based on these outcomes, CDK4/6 inhibitors are currently being tested, alone o in combination with other drugs
Cyclin D1 Restrains Oncogene-Induced Autophagy by Regulating the AMPK-LKB1 Signaling Axis
Casimiro MC, et al.
Cancer Research, 77(13), 3391-3405 (2017)
Craig P Giacomini et al.
PLoS genetics, 9(4), e1003464-e1003464 (2013-05-03)
Gene fusions, like BCR/ABL1 in chronic myelogenous leukemia, have long been recognized in hematologic and mesenchymal malignancies. The recent finding of gene fusions in prostate and lung cancers has motivated the search for pathogenic gene fusions in other malignancies. Here
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