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Merck
모든 사진(1)

주요 문서

PZ0199

Sigma-Aldrich

PD 0332991 isethionate

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

동의어(들):

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

실험식(Hill 표기법):
C24H29N7O2 · C2H6O4S
CAS Number:
Molecular Weight:
573.66
MDL number:
UNSPSC 코드:
12352200
PubChem Substance ID:
NACRES:
NA.77

제품명

PD 0332991 isethionate, ≥98% (HPLC)

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

H2O: 5 mg/mL, clear

저장 온도

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

유전자 정보

애플리케이션

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

생화학적/생리학적 작용

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.

특징 및 장점

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

기타 정보

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.

픽토그램

Skull and crossbones

신호어

Danger

유해 및 위험 성명서

Hazard Classifications

Acute Tox. 3 Oral

Storage Class Code

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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문서 라이브러리 방문

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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