CUDC-907

Catalog No.S2759

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. Phase 1.

Size Price Stock Quantity  
In DMSO USD 550 In stock
USD 270 In stock
USD 370 In stock
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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. Phase 1.
Targets
HDAC1 [1] HDAC3 [1] HDAC10 [1] HDAC2 [1] HDAC11 [1]
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

Solubility (25°C)

In vitro DMSO 102 mg/mL (200.57 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 508.55
Formula

C23H24N8O4S

CAS No. 1339928-25-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02909777 Recruiting Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor Dana-Farber Cancer Institute|Curis, Inc. October 2016 Phase 1
NCT02674750 Recruiting Relapsed and/or Refractory Diffuse Large B-cell Lymphoma Curis, Inc. January 2016 Phase 2
NCT02307240 Recruiting NUT Midline Carcinoma|Breast Cancer|Solid Tumors Curis, Inc. November 2014 Phase 1
NCT01742988 Recruiting Multiple Myeloma|Lymphoma Curis, Inc.|The Leukemia and Lymphoma Society December 2012 Phase 1
NCT03002623 Recruiting Thyroid Neoplasms|Poorly Differentiated and Undifferentiated Thyroid Cancer|Differentiated Thyroid Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) December 16, 2016 Phase 2

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID