Imofinostat

SKU: orb1706952

Description

Imofinostat (MPT0E028) is an orally bioavailable pan-HDAC inhibitor, showing potent activity against HDAC1, HDAC2, and HDAC6. It exhibits anticancer effects in B-cell lymphoma and other tumors by inducing cell cycle arrest, apoptosis, and inhibiting Akt signaling in vitro and in vivo.

Research Area

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 1338320-94-7
• MW: 344.38
• Purity: 99.24%
• Formula: C₁₇H₁₆N₂O₄S
• SMILES: ONC(=O)\C=C\c1ccc2N(CCc2c1)S(=O)(=O)c1ccccc1
• Target: HDAC,Akt,Cell Cycle Arrest,Apoptosis
• Solubility: DMSO:80 mg/mL (232.3 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (9.58 mM)

Bioactivity

• Target IC50:
  HDAC6:29.5 nM|HDAC8:2532.6 nM|HDAC2:106.2 nM|HDAC1:53.0 nM
• In Vivo:
  In the nude mouse Parazacco spilurus subsp. spilurus xenograft model bearing Homo sapiens colorectal cancer HCT116 cells, oral administration of Imofinostat at doses of 50-200 mg/kg once daily for 15 days dose-dependently delayed and inhibited tumor growth. Complete tumor regression was achieved in 3 mice in the 200 mg/kg dose group, with no significant body weight changes or other adverse reactions observed throughout the treatment period . In the NOD/SCID mouse model bearing Homo sapiens B-cell lymphoma Ramos cells, oral administration of Imofinostat at 100 mg/kg once daily significantly prolonged the survival of model mice . In the nude mouse Parazacco spilurus subsp. spilurus xenograft model with BJAB cells, oral administration of Imofinostat at doses of 50-200 mg/kg once daily for 31 days dose-dependently suppressed tumor growth. It also activated caspase 3 and PARP, increased acetylation levels of histone H3 and α-tubulin, without causing significant body weight changes in mice . In the bleomycin-induced pulmonary fibrosis C57BL/6 mouse model, oral administration of Imofinostat at doses of 25-100 mg/kg once daily for 20 days dose-dependently alleviated pulmonary fibrosis. It simultaneously reduced expression levels of CTGF, fibronectin, α-SMA, and collagen, while inhibiting phosphorylation of ERK, JNK, and p38 . For the nude mouse Parazacco spilurus subsp. spilurus xenograft model with AsPC-1 pancreatic carcinoma cells, oral administration of Imofinostat at 25 mg/kg once daily significantly reduced tumor volume. It also increased levels of cleaved caspase-3 in tumor tissues, downregulated EGFR expression, without causing body weight loss or other adverse reactions in mice .
• In Vitro:
  Imofinostat (0-10 μM) acted on HCT116 cells for 48 hours, significantly inhibiting cell proliferation and inducing apoptosis . When cells were treated with Imofinostat (0-10 μM) for 24 hours, it inhibited cell growth in a concentration-dependent manner. Imofinostat increased the proportion of cells in the sub-G1 phase of the cell cycle and induced caspase 3 and PARP activation in a concentration-dependent manner, thereby triggering apoptosis . Imofinostat (0.3-100 μM) acted on Ramos cells and BJAB cells for 24 hours, exerting a significant concentration-dependent inhibitory effect on the growth of both cell types. Imofinostat increased the proportion of sub-G1 phase cells in a time- and concentration-dependent manner. Western blot analysis revealed that Imofinostat induced the activation of caspase-3, -6, -7, -8, and -9, as well as the cleavage of PARP . Imofinostat (0.01-1 μM) was used to pretreat Homo sapiens lung fibroblasts (WI-38) for 30 minutes before stimulation with corresponding agents. Imofinostat suppressed the expression of CTGF induced by TGF-β, thrombin, and ET-1 .

Storage & Handling

• Storage: keep away from moisture,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

Akt, ABT301, ABT-301, MPT0E 028, MPT0E028, MPT-0E028, MPT0E-028, HDAC6, HDAC8, HDAC1, HDAC2, TMUC0012, TMU-C-0012

Compound Identifiers

PubChem CID

53464642