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Merck

PZ0199

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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A propos de cet article

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

Principaux documents

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Nom du produit

PD 0332991 isethionate, ≥98% (HPLC)

SMILES string

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)

InChI key

LYYVFHRFIJKPOV-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 5 mg/mL, clear

storage temp.

room temp

Quality Level

100

Gene Information

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

Catégories apparentées

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

Biochem/physiol Actions

PD 0332991 is a potent selective inhibitor of CDK4 and CDK6.
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.

Features and Benefits

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

Other Notes

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.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Classe de stockage

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000508974
0000508974
0000338689
0000338689
0000245897

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Consulter la Bibliothèque de documents

Checkpoint Controls and Targets in Cancer Therapy, 141-141 (2010)
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
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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