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CDK&Aurora kinase

Palbociclib (PD-0332991) HCl (827022-32-2)

PD0332991 is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Not Intended for Therapeutic Use. For research use only.

CAS: 827022-32-2 Category

Palbociclib (PD-0332991) HCl (827022-32-2) Description

Palbociclib, also known as PD0332991, is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. PD-0332991 selectively inhibits cyclin-dependent kinases (particularly Cdk4/cyclin D1 kinase), which may inhibit retinoblastoma (Rb) protein phosphorylation; inhibition of Rb phosphorylation prevents Rb-positive tumor cells from entering the S phase of the cell cycle (arrest in the G1 phase), resulting in suppression of DNA replication and decreased tumor cell proliferation. PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) (IC50 = 0.011 μmol/L) and Cdk6 (IC50 = 0.016 μmol/L), having no activity against a panel of 36 additional protein kinases. Palbociclib was approved on 2/3/2015 for treatment of advanced (metastatic) breast cancer.

 

Palbociclib (PD-0332991) HCl (827022-32-2) Specifications

Product Name Palbociclib (PD-0332991) HCl
Synonyms PD 0332991; PD-0332991; PD0332991; PD0332991; PD332991; PD-332991; PD 332991; Palbociclib, brand name: Ibrance
Chemical Names 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
Purity ≥98% (HPLC)
CAS Number 827022-32-2
Molecular Formula C24H29N7O2
Molecular Weight 483.99
Monoisotopic Mass 483.215 g/mol
MDL number N/A
InChIKey STEQOHNDWONVIF-UHFFFAOYSA-N
InChi Code InChI=1S/C24H29N7O2.ClH/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);1H
SMILES O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(N4CCNCC4)C=C3)N=C2N1C5CCCC5.[H]Cl
Form Powder
Color Yellow solid
Solubility  Soluble in water and ethanol; slightly soluble in DMSO with warm.
Storage Temp.  −20°C
Shelf life >2 years if stored properly.
Handling Protect from air and light
Application A highly selective inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. L’Allemain G. [Doubling time of progression-free survival by palbociclib in metastatic breast cancer]. Bull Cancer. 2015 Apr;102(4):300. doi: 10.1016/j.bulcan.2015.02.011. French. PubMed PMID: 26042255.

[2]. Palbociclib Extends Survival in Advanced Breast Cancer. Cancer Discov. 2015 Jun 2. [Epub ahead of print] PubMed PMID: 26036642.

[3]. Turner NC, Ro J, André F, Loi S, Verma S, Iwata H, Harbeck N, Loibl S, Huang Bartlett C, Zhang K, Giorgetti C, Randolph S, Koehler M, Cristofanilli M. Palbociclib in Hormone-Receptor-Positive Advanced Breast Cancer. N Engl J Med. 2015 Jun 1. [Epub ahead of print] PubMed PMID: 26030518.

[4].: Niesvizky R, Badros AZ, Costa LJ, Ely SA, Singhal SB, Stadtmauer EA, Haideri NA, Yacoub A, Hess G, Lentzsch S, Spicka I, Chanan-Khan AA, Raab MS, Tarantolo S, Vij R, Zonder JA, Huang X, Jayabalan D, Di Liberto M, Huang X, Jiang Y, Kim ST, Randolph S, Chen-Kiang S. Phase 1/2 study of cyclin-dependent kinase (CDK)4/6 inhibitor palbociclib (PD-0332991) with bortezomib and dexamethasone in relapsed/refractory multiple myeloma. Leuk Lymphoma. 2015 May 15:1-9. [Epub ahead of print] PubMed PMID: 25813205.

[5]. Dhillon S. Palbociclib: first global approval. Drugs. 2015 Apr;75(5):543-51. doi: 10.1007/s40265-015-0379-9. PubMed PMID: 25792301.