Fimepinostat

SKU: orb1306535

Description

Fimepinostat (CUDC-907) is an oral dual inhibitor targeting PI3K class I and HDAC enzymes, disrupting the oncogenic PI3K/AKT/mTOR pathway. It has demonstrated antitumor activity in preclinical models of hematologic and solid tumors, supporting its investigation in both in vitro and in vivo cancer research.

Research Area

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

Key Properties

• CAS Number: 1339928-25-4
• MW: 508.55
• Purity: 99.87% (May vary between batches)
• Formula: C₂₃H₂₄N₈O₄S
• SMILES: COc1ccc(cn1)-c1nc(N2CCOCC2)c2sc(CN(C)c3ncc(cn3)C(=O)NO)cc2n1
• Target: HDAC,PI3K,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.49 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:62.5 mg/mL (122.9 mM)

Bioactivity

• Target IC50:
  HDAC6:27 nM|PI3Kγ:311 nM|PI3Kβ:54 nM|HDAC3:1.8 nM|PI3Kα:19 nM|HDAC8:191 nM|HDAC10:2.8 nM|HDAC11:5.4 nM|HDAC9:554 nM|HDAC7:426 nM|PI3Kδ:39 nM|HDAC5:674 nM|HDAC2:5.0 nM|HDAC1:1.7 nM|HDAC4:409 nM
• In Vivo:
  CUDC-907 exhibits inhibitory effects on the growth of a range of B-cell lymphomas, as demonstrated by its IC50 values in various cell lines including Granta 519 (7 nM), DOHH2 (1 nM), RL (2 nM), Pfeiffer (4 nM), SuDHL4 (3 nM), Daudi (15 nM), and Raji (9 nM). Additionally, CUDC-907 blocks the proliferation of multiple myeloma cell lines such as RPMI8226 (2 nM), OPM-2 (1 nM), and ARH77 (5 nM), indicating its potent anticancer activity against both multiple myeloma and B-cell lymphomas. CUDC-907 also inhibits various PI3K isoforms, including PI3Kβ/γ/δ and PI3KαE545K, with IC50 values of 54, 311, 39, and 62 nM, respectively. Furthermore, it effectively inhibits HDAC isoforms HDAC1/2//6/11 with IC50 values of 191, 27, and 5.4 nM, respectively, plus exhibits mild inhibitory effects on other HDAC enzyme activities.
• In Vitro:
  In studies assessing the efficacy of NHL and MM models, CUDC-907, when administered at its maximum tolerated dose (MTD), demonstrated significantly greater effectiveness compared to either PI3K or HDAC inhibitors alone or their combination. Additionally, CUDC-907 exhibited superior efficacy over the PI3Kδ selective inhibitor CAL-101 at its MTD. It also displayed oral bioavailability in canine species and a longer half-life in murine tumor models. When targeting xenograft tumors, CUDC-907 induced apoptosis and inhibited cancer cell proliferation.
• Cell Research:
  CUDC-907 is dissolved in DMSO and stored (-80°C), and then diluted with appropriate medium before use. Human cancer cell lines are plated at densities of 5,000 to 10,000 per well in 96-well flat-bottomed plates with the recommended culture medium. The cells are then incubated with compounds (e.g.,CUDC-907) at various concentrations for 72 hours in culture medium supplemented with 0.5% (v/v) FBS. Growth inhibition is assessed by assay of cellular ATP content using the Perkin-Elmer ATPlite kit.

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

PI3K, PI3K/HDAC Inhibitor, Phosphoinositide 3-kinase, inhibit, Inhibitor, Histone deacetylases, HDAC, HDAC3, HDAC11, HDAC1, HDAC10, HDAC2, Fimepinostat, CUDC 907, CUDC907, CUDC-907, Apoptosis

Compound Identifiers

PubChem CID

54575456