Fimepinostat (CUDC-907)

Catalog No.S2759

For research use only.

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.

Fimepinostat (CUDC-907) Chemical Structure

CAS No. 1339928-25-4

Selleck's Fimepinostat (CUDC-907) has been cited by 29 publications

Purity & Quality Control

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Glioma cells (HF2885) NVnib4NoS3m2b4TvfIlkcXS7IHHzd4F6 MVm3NkBp NFLWdplEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIdGmxbXGgZ4VtdHNiKFjGNlg5PSliYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRmekeubzDhd5NigSxiRVO1NF0xNjdibl2= NIPWSYk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK4PFY6QSd-Mk[yPFg3QTl:L3G+
human Glioma cells (HF3013) M1ztRWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1[1[lczKGh? NGi4eppEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIdGmxbXGgZ4VtdHNiKFjGN|AyOyliYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRmekeubzDhd5NigSxiRVO1NF0xNjdibl2= NVzXNFR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
human Glioma cells (HF2876)  MX7DfZRwfG:6aXPpeJkh[XO|YYm= M4DYb|czKGh? NIfwVGxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIdGmxbXGgZ4VtdHNiKFjGNlg4PiliYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRmekeubzDhd5NigSxiRVO1NF0xNjdibl2= NVzDc5hNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
human Glioma cells (HF2790)  MkLyR5l1d3SxeHnjbZR6KGG|c3H5 NFHJNIM4OiCq M2\BUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yO|kxMSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= M13m[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mki4Olk6Lz5{NkK4PFY6QTxxYU6=
human Glioma cells (HF2476) MoHCR5l1d3SxeHnjbZR6KGG|c3H5 NXTM[IZOPzJiaB?= M2nZXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yOFc3MSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= M3n0SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mki4Olk6Lz5{NkK4PFY6QTxxYU6=
human Glioma cells (HF2381) MYPDfZRwfG:6aXPpeJkh[XO|YYm= MmTjO|IhcA>? MlriR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS4xqd22jIHPlcIx{KCiKRkKzPFEqKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZJIdG9iYYPzZZktKEWFNUC9NE44KG6P NFjX[XQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK4PFY6QSd-Mk[yPFg3QTl:L3G+
human Glioma cells (HF2303) M2L3O2N6fG:2b4jpZ4l1gSCjc4PhfS=> NWHVUIx7PzJiaB?= NWHJc2JoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlI{ODNrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N NUTOTldkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
MV4-11 MWTDfZRwfG:6aXPpeJkh[XO|YYm= Ml3XNlQhcHK| NIXrUGtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygQVAvODByNEROwG0v MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF6Nk[3Okc,OjdzOE[2O|Y9N2F-
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HCT116 M3;sSGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn3hNlQhcHK| M1TIfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7LDC9NE4xODd|NN88UU4> M4S3bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUi2Olc3Lz5{N{G4OlY4PjxxYU6=
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DU145 NGmwfY5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4PO[Fk3KGi{cx?= M{P3SmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgZYZ1\XJiOU[gbJJ{KGK7IF3UWEBie3OjeTygQVAvPTcQvF2u NEjScXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUGxO|UyPyd-M{GxNVc2OTd:L3G+
HuH7 NWLpWoRRSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NEP0PGM6PiCqcoO= M1XKOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIXIO{Bk\WyuczDh[pRmeiB7NjDodpMh[nliTWTUJIF{e2G7LDC9NE42Ps7:TT6= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTFzN{WxO{c,OzFzMUe1NVc9N2F-
MV4-11 NIfWN|lCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3vvZVI2KHSxIEWwJI5O NH3rZoQ4OiCqcoO= M2XnU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0MVEyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjdDCyOUB1dyB3MDDuUUBi\nSncjC3NkBpenNiYomgeJJ6eGijbjDicJVmKGG|c3H5 NVzXOG4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{KyNVI4OzBpPkOyNlEzPzNyPD;hQi=>
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 ; p-PRAS40 / p-4EBP1 / p-S6 / c-Myc / Cleaved PARP / Caspase-3 / Celaved caspase-3 ; SYK / BTK / Bcl-10 / MyD88 / IRAK4 30353642 28147336
Immunofluorescence γ-H2AX / 53BP1 ; RAD51 29760046
Growth inhibition assay Cell viability 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 (from reference)

Animal Research:

[1]

  • Animal Models: NHL and MM models in mice
  • Dosages: 100 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 508.55
Formula

C23H24N8O4S

CAS No. 1339928-25-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02909777 Recruiting Drug: CUDC-907 Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor Dana-Farber Cancer Institute|Curis Inc. October 2016 Phase 1
NCT02307240 Completed Drug: CUDC-907 Triple-Negative Breast Cancer|High-grade Serous Ovarian Cancer|Solid Tumors|NUT Midline Carcinoma Curis Inc. November 2014 Phase 1
NCT01742988 Completed Drug: fimepinostat|Drug: Rituximab|Drug: venetoclax Lymphoma|Relapsed Lymphoma|Refractory Lymphoma|Relapsed and/or Refractory Lymphoma|Relapsed Ddiffuse Large B-Cell Lymphoma (DLBCL)|Refractory Diffuse Large B-Cell Lymphoma (DLBCL)|Relapsed and/or Refractory Diffuse Large B-Cell Lymphoma (DLBCL)|Double-hit Lymphoma (DHL)|Triple-hit Lymphoma (THL)|Double-expressor Lymphoma (DEL)|High-grade B-cell Lymphoma (HGBL) Curis Inc.|The Leukemia and Lymphoma Society December 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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