For research use only.
CAS No. 1339928-25-4
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.
Selleck's Fimepinostat (CUDC-907) has been cited by 20 publications
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|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.|
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.  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. 
|In vivo||CUDC-907 has a long half-life in murine tumors. CUDC-907 induces apoptosis and inhibits cancer cell proliferation in xenograft tumors.  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. |
|In vitro||DMSO||102 mg/mL (200.57 mM)|
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Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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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|
|NCT02674750||Completed||Drug: CUDC-907||Relapsed and/or Refractory Diffuse Large B-cell Lymphoma Including With Myc Alterations||Curis Inc.||January 2016||Phase 2|
|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||Active not recruiting||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|
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.
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Frequently Asked Questions
How to solve CUDC-907 for in vivo studies (p.o.)?
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.
What is the half-life of CUDC-907 in vivo?
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.