PZ0199

PD 0332991 isethionate

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

• Synonym(e): 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
• Empirische Formel (Hill-System): C₂₄H₂₉N₇O₂ · C₂H₆O₄S
• CAS-Nummer: 827022-33-3
• Molekulargewicht: 573.66
• UNSPSC Code: 12352200
• PubChem Substance ID: 329823771
• NACRES: NA.77
• MDL number: MFCD22666589
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Produktname: PD 0332991 isethionate, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: H₂O: 5 mg/mL, clear
• storage temp.: room temp
• 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
• Gene Information: human ... CCND1(595), CDK4(1019), CDK6(1021)

Beschreibung

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.

Sicherheitshinweise

• Piktogramme: GHS08,GHS09
• Signalwort: Warning
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable
• Zielorgane: Bone marrow,male reproductive organs
• Gefahrencodes: H341,H361f,H373,H411
• Sicherheitshinweise: P202 - P260 - P273 - P280 - P308 + P313 - P391
• Hazard Classifications: Aquatic Chronic 2 - Muta. 2 - Repr. 2 - STOT RE 2 Oral
• Lagerklasse: 11 - Combustible Solids