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PZ0383

Sigma-Aldrich

Palbociclib

≥98% (HPLC), powder, CDK 4 & 6 inhibitor

Synonyme(s) :

6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one, Ibrance, PD 0332991, PD 332991, PD-0332991, PD0332991, PD991, PF 00080665, PF-00080665, PF00080665

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About This Item

Formule empirique (notation de Hill):
C24H29N7O2
Numéro CAS:
571190-30-2
Poids moléculaire :
447.53
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Nom du produit

Palbociclib, ≥98% (HPLC)

Essai

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

0.1 M HCl: 2 mg/mL, clear

Température de stockage

room temp

Chaîne SMILES 

CC(C1=C(N2C3CCCC3)N=C(NC4=CC=C(N5CCNCC5)C=N4)N=C1)=C(C(C)=O)C2=O

InChI

1S/C24H29N7O2/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/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29)

Clé InChI

AHJRHEGDXFFMBM-UHFFFAOYSA-N

Actions biochimiques/physiologiques

PF-00080665 (Palbociclib; PD 0332991) is an orally active and highly specific inhibitor against cyclin-dependent kinase 4 & 6 (IC50 = 9, 11, 15 nM, respectively, using CDK4/cycD3, CDK4/cycD1, CDK6/cycD2; IC50 >10 μM against 36 other kinases) that potently suppresses Cdk4/6-dependent cellular Rb phosphorylation (IC50 = 66 nM/pSer780 & 63 nM/pSer795; MDA-MB-435). PF-00080665 exhibits selective antiproliferation activity against Rb-positive human breast/colon/lung/leukemia cancer cultures (IC50 = 40-400 nM; IC50 >3 μM/Rb-negative MDA-MB-468 & H2009) and displays in vivo efficacy against various advanced stage human tumor xenografts in mice (12.5-150 mg/kg/day p.o.).

Stockage et stabilité

This chemical can be stored in solution at -80°C for 6 months and at -20°C for 1 month (protect from light).

Pictogrammes

Health hazardEnvironment
GHS08,GHS09

Mention d'avertissement

Warning

Mentions de danger

H341,H361f,H373,H411

Classification des risques

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

Organes cibles

Bone marrow,male reproductive organs

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000340107
0000248341
0000248340
0000340107
0000248340

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Max Heckler et al.
Cancer discovery, 11(10), 2564-2581 (2021-05-05)
CDK4/6 inhibitors are approved to treat breast cancer and are in trials for other malignancies. We examined CDK4/6 inhibition in mouse and human CD8+ T cells during early stages of activation. Mice receiving tumor-specific CD8+ T cells treated with CDK4/6
The anti-tumor efficacy of CDK4/6 inhibition is enhanced by the combination with PI3K/AKT/mTOR inhibitors through impairment of glucose metabolism in TNBC cells.
Daniele Cretella et al.
Journal of experimental & clinical cancer research : CR, 37(1), 72-72 (2018-03-29)
E Martínez de Dueñas et al.
Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico (2018-03-23)
Cyclin-dependent kinases (CDKs) play a key role in cell cycle regulation, which makes them a clear therapeutic target to interfere with cell division and proliferation in cancer patients. Palbociclib, a specific inhibitor of CDK4/6 with outstanding clinical efficacy data and
ER
Angel L Guerrero-Zotano et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 24(11), 2517-2529 (2018-03-28)
Shinya Kitamura et al.
Cancer science, 113(2), 802-807 (2021-12-07)
Extramammary Paget's disease (EMPD) is a rare adnexal neoplasm commonly seen in the genital areas among the senior population. The prognosis of advanced EMPD is not favorable; thus, the development of potential treatments has long been sought. Cyclin-dependent kinase (CDK)
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