Palbociclib

SKU: orb1307454

Description

Palbociclib is an orally bioavailable, potent inhibitor of CDK4 and CDK6 (IC50 11/16 nM) with anti-tumor activity. It is widely investigated in preclinical in vitro and in vivo studies for ER-positive, HER2-negative breast cancer and other cyclin D-driven malignancies.

Research Area

Cell Biology

Key Properties

• CAS Number: 571190-30-2
• MW: 447.53
• Purity: 98.02%
• Formula: C₂₄H₂₉N₇O₂
• SMILES: O=C1N(C=2C(C(C)=C1C(C)=O)=CN=C(NC3=CC=C(C=N3)N4CCNCC4)N2)C5CCCC5
• Target: CDK
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble);0.1 M HCL:1.25 mg/mL (2.79 mM);Ethanol:insoluble

Bioactivity

• Target IC50:
  MAPK:8000 nM|DYRK1A:2000 nM|CDK4:11 nM|ICNI cells:8 µM|CDK6:16 nM|KB-C2 cells:22.573 µM|CDK4-CyclinD3:9 nM|CDK6-CyclinD2:16 nM|CDK4-CyclinD1:11 nM
• In Vivo:
  METHODS: To detect antitumor activity in vivo, Palbociclib (12.5-150 mg/kg, sodium lactate buffer (50 mmol/L, pH 4.0)) was administered orally to immunodeficient mice harboring the tumors Colo-205 or MDA-MB-435 once daily for fourteen days. RESULTS: Palbociclib showed significant anti-tumor efficacy in multiple human tumor xenograft models. In Colo-205 tumors, PD 0332991 administered for 14 days produced rapid tumor regression. METHODS: To assay antitumor activity in vivo, Palbociclib (150 mg/kg, sodium lactate buffer (50 mM, pH = 4.0)) was administered once daily for two weeks by gavage to nu/nu BALB/c mice bearing esophageal squamous cell carcinoma (ESCC) tumors EC109 or KYSE150. RESULTS: Palbociclib effectively inhibited ESCC tumor growth and lung metastasis.
• In Vitro:
  METHODS: Malignant rhabdomyosarcoma cells G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) were treated with Palbociclib (0-1 mM) for 24 h, and cell viability was assayed by WST. RESULTS: Palbociclib effectively inhibited AN, RY, G401 and NS cell lines in a concentration-dependent manner, with IC50s of 0.01 μM, 0.01 μM, 0.06 μM and 0.6 μM, respectively; on the contrary, the YM cell line was resistant to Palbociclib, with an IC50 >10 μM. METHODS: Human breast cancer cells MDA-MB-453 were treated with Palbociclib (0.02-10 μmol/L) for 24 h, and the cell cycle was examined by Flow Cytometry. RESULTS: Palbociclib caused G1 phase block.
• Cell Research:
  Palbociclib (PD) is prepared in DMSO and stored ( 80°C), and then diluted with appropriate media before use. MRT cell lines, G401, MP-MRT-AN (AN), KP-MRT-RY (RY), KP-MRT-NS (NS), and KP-MRT-YM (YM) cell lines are seeded in normal growth medium into 96-well cell plates. After 24 h, the culture medium is replaced with culture medium containing Palbociclib (0.05 or 1 μM) or DMSO. Cells are cultured and treated in triplicate. Cell proliferation is determined 8 days after the treatment by WST-8 assay using a Cell Counting Kit-8.

Storage & Handling

• Storage: keep away from direct sunlight | 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

CDK6, CDK4, cell cycle, Breast cancer, CDK, Cyclin dependent kinase, inhibit, PD0332991, PD-0332991, PD 0332991, Palbociclib, estrogen receptor, Inhibitor, HER2, hepatocellular carcinoma, HCC

Compound Identifiers

PubChem CID

5330286