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PZ0199

Sigma-Aldrich

PD 0332991 isethionate

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

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C24H29N7O2 · C2H6O4S
Numero CAS:
Peso molecolare:
573.66
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

product name

PD 0332991 isethionate, ≥98% (HPLC)

Livello qualitativo

Saggio

≥98% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

H2O: 5 mg/mL, clear

Temperatura di conservazione

room temp

Stringa SMILE

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)
LYYVFHRFIJKPOV-UHFFFAOYSA-N

Informazioni sul gene

Applicazioni

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

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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

Altre note

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.

Pittogrammi

Skull and crossbones

Avvertenze

Danger

Indicazioni di pericolo

Classi di pericolo

Acute Tox. 3 Oral

Codice della classe di stoccaggio

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

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (COA)

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Cyclin D1 Restrains Oncogene-Induced Autophagy by Regulating the AMPK-LKB1 Signaling Axis
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Cancer Research, 77(13), 3391-3405 (2017)
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Articoli

Review properties, activators and inhibitors, and available products for researching cyclin-dependent kinases (CDKs).

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