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Fimepinostat

Catalog No. T2078 CAS 1339928-25-4

Synonyms: CUDC-907, PI3K/HDAC Inhibitor, CUDC 907

Fimepinostat (CUDC 907) is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types.

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Fimepinostat, CAS 1339928-25-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 185.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 538.00
500 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 99.87%

Purity: 99.66%

Purity: 99.23%

Purity: 97.13%

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Storage & Solubility Information

Description	Fimepinostat (CUDC 907) is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types.
Targets&IC50	HDAC1:1.7 nM, HDAC10:2.8 nM, HDAC11:5.4 nM, HDAC3:1.8 nM, HDAC2:5.0 nM
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.
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.
Kinase Assay	The activities of classes I and II HDACs are measured using the Color-de-Lys assay system. The activity of PI3K is measured using the ADP-Glo luminescent kinase assay. Recombinant PI3K protein, a complex of N-terminal GST-tagged recombinant full-length human p110 and untagged recombinant full-length human p85, is coexpressed in a baculovirus-infected Sf9 cell expression system[1].
Cell Research	CUDC-907 is dissolved in DMSO and stored (-80°C), and then diluted with appropriate medium before use[1]. 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[1].

Synonyms	CUDC-907, PI3K/HDAC Inhibitor, CUDC 907
Molecular Weight	508.55
Formula	C23H24N8O4S
CAS No.	1339928-25-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 94 mg/mL (184.8 mM)

References and Literature

1. Qian C, et al. Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling. Clin Cancer Res. 2012 Aug 1;18(15):4104-13.

Citations

1. Li M, Hu Y, Wang J, et al.The dual HDAC and PI3K inhibitor, CUDC‑907, inhibits tumor growth and stem‑like properties by suppressing PTX3 in neuroblastoma.International Journal of Oncology.2024, 64(2): 1-13.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Obesity Compound Library Cancer Cell Differentiation Compound Library Anti-Ovarian Cancer Compound Library Bioactive Compounds Library Max

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Keywords

Fimepinostat 1339928-25-4 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair PI3K/Akt/mTOR signaling PI3K HDAC CUDC-907 CUDC907 inhibit PI3K/HDAC Inhibitor Inhibitor CUDC 907 Phosphoinositide 3-kinase Histone deacetylases inhibitor

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