PZ0383

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

Properties

• 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

Description

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).

Safety Information

• Pictograms: GHS08,GHS09
• Signal Word: Warning
• Hazard Statements: H341,H361f,H373,H411
• Precautionary Statements: P202 - P260 - P273 - P280 - P308 + P313 - P391
• 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