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PZ0383

Sigma-Aldrich

Palbociclib

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

Synonym(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

Empirical Formula (Hill Notation):
C24H29N7O2
CAS Number:
571190-30-2
Molecular Weight:
447.53
UNSPSC Code:
12352200
NACRES:
NA.77

Product Name

Palbociclib, ≥98% (HPLC)

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

0.1 M HCl: 2 mg/mL, clear

storage temp.

room temp

SMILES string

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)

InChI key

AHJRHEGDXFFMBM-UHFFFAOYSA-N

Biochem/physiol Actions

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.).

Storage and Stability

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

Pictograms

Health hazardEnvironment
GHS08,GHS09

Signal Word

Warning

Hazard Statements

H341,H361f,H373,H411

Hazard Classifications

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

Target Organs

Bone marrow,male reproductive organs

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000340107
0000248340
0000248341
0000204248
0000184242

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Fiona J Ruiz et al.
Cancers, 13(18) (2021-09-29)
Cervical cancer tumors with undetectable HPV (HPVU) have been underappreciated in clinical decision making. In this study, two independent CC datasets were used to characterize the largest cohort of HPVU tumors to date (HPVU = 35, HPV+ = 430). Genomic
Xiaoyang Li et al.
Cell death & disease, 9(5), 446-446 (2018-04-20)
Synovial sarcoma is a highly aggressive but rare form of soft tissue malignancy that primarily affects the extremities of the arms or legs, for which current chemotherapeutic agents have not been proven to be very effective. The cyclin-dependent kinase 4/6-retinoblastoma
Ryohei Kozaki et al.
Cancers, 10(4) (2018-04-25)
Bruton's tyrosine kinase (BTK) is a key regulator of the B-cell receptor signaling pathway, and aberrant B-cell receptor (BCR) signaling has been implicated in the survival of malignant B-cells. However, responses of the diffuse large B-cell lymphoma (DLBCL) to inhibitors
Flora Doffe et al.
Cancers, 14(15) (2022-07-28)
The recent trend in 3D cell modeling has fostered the emergence of a wide range of models, addressing very distinct goals ranging from the fundamental exploration of cell-cell interactions to preclinical assays for personalized medicine. It is clear that no
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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