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CUDC-907

Cat. No. M2111
CUDC-907 Structure
Size Price Availability Quantity
10mg USD 229 In stock
50mg USD 648 In stock
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Quality Control
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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 508.55
Formula C23H24N8O4S
CAS Number 1339928-25-4
Purity >99%
Solubility DMSO
Storage at -20°C
References

Cancer network disruption by a single molecule inhibitor targeting both histone deacetylase activity and phosphatidylinositol 3-kinase signaling.
Qian C, et al. Clin Cancer Res. 2012 Aug 1;18(15):4104-13. PMID: 22693356.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CUDC-907 supplier, HDAC, inhibitors

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