Palbociclib Isethionate

SKU: orb1300947

Description

Palbociclib Isethionate (PD 0332991 isethionate) is a potent and selective CDK4/6 inhibitor with IC50 values of 11 and 16 nM, respectively, and demonstrates high selectivity across kinases. It is widely used in cancer research, particularly for studying cell cycle arrest in breast cancer models, both in vitro and in vivo.

Research Area

Cell Biology

Key Properties

• CAS Number: 827022-33-3
• MW: 573.66
• Purity: 99.85% (May vary between batches)
• Formula: C₂₄H₂₉N₇O₂·C₂H₆O₄S
• SMILES: OCCS(O)(=O)=O.CC(=O)c1c(C)c2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n(C2CCCC2)c1=O
• Target: CDK
• Solubility: DMSO:40 mg/mL (69.73 mM);H2O:57.4 mg/mL (100.06 mM)

Bioactivity

• Target IC50:
  CDK4-CyclinD3:9 nM (cell free)|CDK4-CyclinD1:11 nM (cell free)|CDK6-CyclinD2:15 nM (cell free)|DYRK1A:2000 nM|MAPK:8000 nM
• In Vivo:
  Oral administration of PD 0332991 to mice bearing the Colo-205 human colon carcinoma produces marked tumor regression. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F .
• In Vitro:
  Palbociclib is a highly specific inhibitor of Cdk4 (IC50, 0.011 micromol/L) and Cdk6 (IC50, 0.016 micromol/L). It is a potent antiproliferative agent against retinoblastoma (Rb)-positive tumor cells in vitro, inducing an exclusive G1 arrest, with a concomitant reduction of phospho-Ser780/Ser795 on the Rb protein . In all of the cell lines except KP-MRT-YM, Palbociclib inhibited cell proliferation >50% (IC50 values 0.01 to 0.6 μM), and induced G1-phase cell cycle arrest. The sensitivity of the MRT cell lines to Palbociclib was inversely correlated with p16 expression. KP-MRT-YM cells overexpress p16 and were resistant to the growth inhibitory effect of Palbociclib . Cell lines representing luminal estrogen receptor-positive (ER+) subtype (including those that are HER2 amplified) were most sensitive to growth inhibition by Palbociclib while nonluminal/basal subtypes were most resistant .
• Cell Research:
  Cells were seeded at 2 × 10^4 per well in a 96-well Cytostar T plate and incubated overnight to allow cells to attach. Varying concentrations of PD 0332991 were added to the wells and incubated for 24 hours at 37°C. [14C]thymidine (0.1 μCi) was added to each well and incorporation of the radiolabel was allowed to proceed for 72 hours. Incorporated radioactivity was determined with a β plate counter .
• Animal Research:
  Mice (18–22 g) were randomized and then implanted s.c. with tumor fragments (～30 mg) into the region of the right axilla. Treatment was initiated when tumors reached 100 to 150 mg. PD 0332991 was given according to the schedule and dose indicated in the table and figure legends by gavage as a solution in sodium lactate buffer (50 mmol/L, pH 4.0) based on mean group body weight. In all experiments, there were 12 mice in the control group and 8 mice each in the treated groups. Additional details for each experiment are given in the table legends .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Palbociclib, Palbociclib (PD0332991) Isethionate, Palbociclib Isethionate, PD0332991, PD-0332991, PD 0332991, PD 0332991 isethionate, hepatocellular carcinoma, HER2, HCC, estrogen receptor, Cyclin dependent kinase, Breast cancer, CDK6/CyclinD2, CDK, CDK4/CyclinD1, CDK4/CyclinD3, cell cycle

Compound Identifiers

PubChem CID

11478676