Panobinostat

SKU: orb1225107

Description

A potent, broad-spectrum HDAC inhibitor with IC50 of 5-20 nM in cell-free assyas; induces cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation, increases mRNA levels of proapoptosis, growth arrest, and DNA damage repair genes including FANCG, FOXO3A, GADD45A, GADD45B, and GADD45G; significantly slows tumor growth derived from Meso and NSCLC cells in vivo models.Blood Cancer Approved(In Vitro):Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta treatment results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells. Panobinostat exhibites potent antiproliferative activity in human NSCLC cell lines with the IC50 ranging from 5 to 100 nM.(In Vivo):Panobinosta (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 404950-80-7
• MW: 349.4262
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₃N₃O₂
• SMILES: O=C(NO)/C=C/C1=CC=C(CNCCC2=C(C)NC3=C2C=CC=C3)C=C1
• Target: HDAC
• Solubility: DMSO: ≥ 57 mg/mL

Bioactivity

• In Vivo:
  Panobinosta (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells In vivo models. Panobinosta markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice. Panobinostat (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model.
• In Vitro:
  Panobinosta (LBH589) induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta treatment results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells. Panobinostat exhibites potent antiproliferative activity in human NSCLC cell lines with the IC50 ranging from 5 to 100 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LBH-589 | LBH589 | NVP-LBH589

Quick Database Links

Gene Symbol

HDAC