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CUDC-907

Cat. No. M2111
CUDC-907 Structure
Synonym:

fimepinostat

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 60  USD60 In stock
5mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

CUDC-907 is an orally-available small molecule inhibitor that targets both HDAC and PI3K with IC50 values of 19 nM, 54 nM, 311 nM and 39 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ respectively. CUDC-907 potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes. CUDC-907 durably inhibits the PI3K-AKT-mTOR pathway and compensatory signaling molecules such as RAF, MEK, MAPK, and STAT-3, as well as upstream receptor tyrosine kinases. CUDC-907 shows greater growth inhibition and proapoptotic activity than single-target PI3K or HDAC inhibitors in both cultured and implanted cancer cells. CUDC-907 is currently in phase I clinical trials for patients with solid tumors or lymphoma.

Customer Product Validations & Biological Datas
Source Stem Cells Dev (2017). Figure 3. CUDC-907
Method Western blot
Cell Lines H3K9ac, H4K8ac, H3K4me2 cell
Concentrations 500 nM
Incubation Time 24 h
Results Interestingly, the combination of both HDAC and PI3K inhibitors failed to induce adipogenesis, suggesting additional possible mechanism by which CUDC-907 promotes adipogenesis
Source Stem Cells Dev (2017). Figure 1. CUDC-907
Method Adipogenic differentiation
Cell Lines hMSCs
Concentrations 500 nM
Incubation Time 24 h
Results CUDC-907 treatment of hBMSCs enhanced adipocyte differentiation, as evidenced by the greater Oil Red O staining and quantitative analysis demonstrated that the number of mature adipocytes identified by Nile red staining was higher.
Protocol (for reference only)
Cell Experiment
Cell lines BT474, N87, H1975, H1993, Calu-6, H460 cells line
Preparation method Cancer cell growth inhibition assay Human cancer cell lines were purchased from American Type Culture Collection (Manassas, VA) and plated at densities of 5,000 to 10,000 per well in 96-well flat-bottomed plates with the recommended culture medium. The cells were then incubated with compounds at various concentrations for 72 hours in culture medium supplemented with 0.5% (v/v) FBS. Growth inhibition was assessed by assay of cellular ATP content using the Perkin-Elmer ATPlite kit.
Concentrations 0~900nM
Incubation time 72 h
Animal Experiment
Animal models Six- to 8-week-old female athymic (nude nu/nu CD-1) or severe combined immunodeficient (SCID) mice Daudi NHL xenograft mouse model
Formulation formulated in 30% Captisol
Dosages 25, 50, and 100 mg/kg
Administration oral gavage
Chemical Information
Molecular Weight 508.55
Formula C23H24N8O4S
CAS Number 1339928-25-4
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Qian C, et al. Clin Cancer Res. Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling.

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Keywords: CUDC-907, fimepinostat supplier, HDAC, inhibitors, activators


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