Fimepinostat(CUDC-907)

For research use only.

Catalog No.S2759

19 publications

Fimepinostat(CUDC-907) Chemical Structure

Molecular Weight(MW): 508.55

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.

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10mM (1mL in DMSO) USD 550 In stock
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Selleck's Fimepinostat(CUDC-907) has been cited by 19 publications

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Choose Selective HDAC Inhibitors

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)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Glioma cells (HF2885) MnT6R5l1d3SxeHnjbZR6KGG|c3H5 MlTXO|IhcA>? M4HKemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yPFg2MSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= NXuz[5c2OjZ{OEi2PVk>
human Glioma cells (HF3013) MmjrR5l1d3SxeHnjbZR6KGG|c3H5 MXO3NkBp M{S0bWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[zNFE{MSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= MlPQNlYzQDh4OUm=
human Glioma cells (HF2876)  MVfDfZRwfG:6aXPpeJkh[XO|YYm= NGrQemM4OiCq NITSbWxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIdGmxbXGgZ4VtdHNiKFjGNlg4PiliYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRmekeubzDhd5NigSxiRVO1NF0xNjdibl2= NID0WnozPjJ6OE[5PS=>
human Glioma cells (HF2790)  MmPHR5l1d3SxeHnjbZR6KGG|c3H5 M1HhPVczKGh? NWT0SZdyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlI4QTBrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N M{\1fVI3Ojh6Nkm5
human Glioma cells (HF2476) M33tdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NEX5[XU4OiCq M2X0[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yOFc3MSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= M2fFdlI3Ojh6Nkm5
human Glioma cells (HF2381) NIqyW2VEgXSxdH;4bYNqfHliYYPzZZk> NULJeIJMPzJiaB?= NX20[IR1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlI{QDFrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N NV7QcpF[OjZ{OEi2PVk>
human Glioma cells (HF2303) M1;6bWN6fG:2b4jpZ4l1gSCjc4PhfS=> MXq3NkBp MmC4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS4xqd22jIHPlcIx{KCiKRkKzNFMqKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZJIdG9iYYPzZZktKEWFNUC9NE44KG6P NGCzRXUzPjJ6OE[5PS=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AKT / p-AKT / P-p70S6K1 / Ac-H3K9 / p-MEK / p-ERK / p-STAT3 / MCL-1 / Bcl-2 / Bcl-xl / PARP; 

PubMed: 30353642     


Western blots showing protein expression in lysates of MEC-1 cells treated with CUDC-907 at various concentrations or DMSO as a control (0) for 12 h. AKT, p-AKT (Ser473), p-p70S6K (Thr389), Ac-H3K9, ERK, p-ERK (Thr202/Tyr204), p-MEK (Ser217/221), STAT3, p-STAT3 (Tyr705), MCL-1, BCL-2, BCL-xL, and PARP were detected with specific antibodies. β-actin was used as a loading control. 

p-PRAS40 / p-4EBP1 / p-S6 / c-Myc / Cleaved PARP / Caspase-3 / Celaved caspase-3 ; 

PubMed: 28147336     


Western blot analysis demonstrating the effect of increasing concentration of CUDC-907 (from 0.01 to 1 μM) on PI3K downstream targets (p4EBP1, pPRAS40 and pS6) and histone H3 acetylation (Ac Histone H3). The actual inhibition of PI3K and HDAC resulted in a decrease in c-Myc protein levels. Activation of caspase 3 and PARP was present as well. 

SYK / BTK / Bcl-10 / MyD88 / IRAK4 ; 

PubMed: 28147336     


Western blot confirming the effect of CUDC-907 (0.1 μM for 24 hours) on BCR and TLR signaling proteins in B-cell lymphoma cell lines (GCB n = 3 and ABC n = 3).

30353642 28147336
Immunofluorescence
γ-H2AX / 53BP1; 

PubMed: 29760046     


Representative images and quantification of immunofluorescence staining for γH2AX and 53BP1 in SF188 cells treated with radiotherapy (4 Gy), CUDC-907 (100 nmol/L), or combination treatment in which radiotherapy was combined with KU70 siRNA, RAD51 siRNA (48 hours after siRNA transfection), or CUDC-907 (16 hours prior to 4 Gy).

RAD51; 

PubMed: 29760046     


Representative images and quantification of immunofluorescence staining for γH2AX and RAD51 in SF188 cells treated with radiotherapy (4 Gy), CUDC-907 (100 nmol/L), or combination treatment in which radiotherapy was combined with KU70 siRNA, RAD51 siRNA (48 hours after siRNA transfection), or CUDC-907 (16 hours prior to 4 Gy).

29760046
Growth inhibition assay
Cell viability; 

PubMed: 28147336     


MTS assay of 8 representative DLBCL and 2 Hodgkin lymphoma cell lines treated with increasing dose of CUDC-907 from 0.01 to 10 μM for 24, 48, 72 hours. Error bars represent standard error of the mean (S.E.M) of triplicate experiments. 

28147336
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

Animal Research:

[1]

- Collapse
  • Animal Models: NHL and MM models in mice
  • Dosages: 100 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 102 mg/mL (200.57 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 508.55
Formula

C23H24N8O4S

CAS No. 1339928-25-4
Storage powder
in solvent
Synonyms N/A
Smiles COC1=CC=C(C=N1)C2=NC3=C(SC(=C3)CN(C)C4=NC=C(C=N4)C(=O)NO)C(=N2)N5CCOCC5

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    How to solve CUDC-907 for in vivo studies (p.o.)?

  • Answer:

    If you decided to take P.O. as your administration route, we suggest you to use 1% CMC-Na to dilute CUDC-907 as a suspension solution for gavage.

  • Question 2:

    What is the half-life of CUDC-907 in vivo?

  • Answer:

    GUDC-907 is said to have a long half-life in mouse tumor model: http://cancerres.aacrjournals.org/content/72/8_Supplement/3744.short, however, its not formally published and we have no detail of how long it is.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID