Fimepinostat (CUDC-907)

Catalog No.S2759 Batch:S275903

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Technical Data

Formula

C23H24N8O4S

Molecular Weight 508.55 CAS No. 1339928-25-4
Solubility (25°C)* In vitro DMSO 102 mg/mL (200.57 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC10 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC11 [1]
(Cell-free assay)
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1.7 nM 1.8 nM 2.8 nM 5.0 nM 5.4 nM
In vitro

CUDC-907 inhibits other PI3K isoforms such as PI3Kβ, PI3Kγ, PI3Kδ, PI3KɑH1047R and PI3KɑE545K with IC50 of 54 nM, 311 nM, 39 nM, 73 nM and 62 nM, respectively. Moreover, CUDC-907 also prevents HDAC subtypes HDAC8, HDAC6 and HDAC11 with IC50 of 191 nM, 27 nM and 5.4 nM, respectively. [1]

In addition, CUDC-907 suppresses other types of HDAC enzymatic activity with lower potency. CUDC-907 inhibits the growth of a series of B cell lymphoma such as Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi and Raji with IC50 of 7 nM, 1 nM, 2 nM, 4 nM, 3 nM, 15 nM and 9 nM, respectively. CUDC-907 also blocks the proliferation of Myeloma including RPMI8226, OPM-2 and ARH77 with IC50 of 2 nM, 1 nM and 5 nM, respectively. CUDC-907 displays greater anti-tumor activity in multiple myeloma and B cell lymphoma. [1]

In vivo

CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors. [1]

In efficacy studies in NHL and MM models, CUDC-907 is more efficacious than either a single-agent PI3K or HDAC inhibitor reference compound or a combination of the two agents given at maximally tolerated doses (MTD). Furthermore, CUDC-907 is more efficacious than the PI3Kδ-selective inhibitor CAL-101 when dosed at MTD doses. [1]

Protocol (from reference)

Animal Study:

[1]

  • Animal Models

    NHL and MM models in mice

  • Dosages

    100 mg/kg

  • Administration

    Administered via p.o.

Customer Product Validation

Data from [Data independently produced by , , Stem Cells Dev, 2017, 26(5):353-362]

Data from [Data independently produced by , , Saudi J Gastroenterol, 2017, 23(1):34-38]

Selleck's Fimepinostat (CUDC-907) has been cited by 35 publications

Multimodal Therapy Approaches for NUT Carcinoma by Dual Combination of Oncolytic Virus Talimogene Laherparepvec with Small Molecule Inhibitors [ Viruses, 2024, 16(5)775] PubMed: 38793657
Reversible epigenetic alterations mediate PSMA expression heterogeneity in advanced metastatic prostate cancer [ JCI Insight, 2023, 8(7)e162907] PubMed: 36821396
Anti-tumor effects of dual PI3K-HDAC inhibitor CUDC-907 on activation of ROS-IRE1α-JNK-mediated cytotoxic autophagy in esophageal cancer [ Cell Biosci, 2022, 12(1):135] PubMed: 35989326
Co-targeting of HDAC, PI3K, and Bcl-2 results in metabolic and transcriptional reprogramming and decreased mitochondrial function in acute myeloid leukemia [ Biochem Pharmacol, 2022, 205:115283] PubMed: 36208684
Utilizing an Endogenous Progesterone Receptor Reporter Gene for Drug Screening and Mechanistic Study in Endometrial Cancer [ Cancers (Basel), 2022, 14(19)4883] PubMed: 36230806
Histone Deacetylase Inhibitors as a Therapeutic Strategy to Eliminate Neoplastic "Stromal" Cells from Giant Cell Tumors of Bone [ Cancers (Basel), 2022, 14(19)4708] PubMed: 36230631
poly(I:C) synergizes with proteasome inhibitors to induce apoptosis in cervical cancer cells [ Transl Oncol, 2022, 18:101362] PubMed: 35151092
The combination of CUDC-907 and gilteritinib shows promising in vitro and in vivo antileukemic activity against FLT3-ITD AML [ Blood Cancer J, 2021, 11(6):111] PubMed: 34099621
Targeting phosphoinositide 3-kinases and histone deacetylases in multiple myeloma [ Exp Hematol Oncol, 2021, 10(1):19] PubMed: 33663586
Antitumor activity and mechanism of resistance of the novel HDAC and PI3K dual inhibitor CUDC-907 in pancreatic cancer [ Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0] PubMed: 33392641

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.