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PZ0199

PD 0332991 isethionate

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

Synonym(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

Empirical Formula (Hill Notation):
C24H29N7O2 · C2H6O4S
CAS Number:
827022-33-3
Molecular Weight:
573.66
UNSPSC Code:
12352200
PubChem Substance ID:
329823771
NACRES:
NA.77
MDL number:
MFCD22666589
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Product Name

PD 0332991 isethionate, ≥98% (HPLC)

Quality Level

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)

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

Health hazardEnvironment
GHS08,GHS09

signalword

Warning

flash_point_f

Not applicable

flash_point_c

Not applicable

target_organs

Bone marrow,male reproductive organs

Hazard Classifications

Aquatic Chronic 2 - Muta. 2 - Repr. 2 - STOT RE 2 Oral

Storage Class

11 - Combustible Solids

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Certificates of Analysis (COA)

Lot/Batch Number
0000508974
0000508974
0000338689
0000338689
0000245897

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Checkpoint Controls and Targets in Cancer Therapy, 141-141 (2010)
Androgen-Sensitized Apoptosis of HPr-1AR Human Prostate Epithelial Cells
Chen C, et al.
PLoS ONE, 11(5), e0156145-e0156145 (2016)
Seizure suppression through manipulating splicing of a voltage-gated sodium channel
Lin WH, et al.
Brain, 138(4), 891-901 (2015)
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