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E7386

Cat. No. M21106
E7386 Structure
Size Price Availability Quantity
5mg USD 320  USD320 In stock
10mg USD 450  USD450 In stock
25mg USD 760  USD760 In stock
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Quality Control & Documentation
Biological Activity

E7386 is an orally active and selective inhibitor of β-catenin/CBP protein interactions and is a key node in the long-studied Wnt/β-catenin cancer pathway.

Chemical Information
Molecular Weight 725.85
Formula C39H48FN9O4
CAS Number 1799824-08-0
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] Toshio Imai, et al. Oncol Lett. Different types of reactions to E7386 among colorectal cancer patient-derived organoids and corresponding CAFs

[2] Yusuke Kanda, et al. Biochem Biophys Res Commun. NF-κB suppression synergizes with E7386, an inhibitor of CBP/β-catenin interaction, to block proliferation of patient-derived colon cancer spheroids

[3] Kazuhiko Yamada, et al. Cancer Res. E7386, a Selective Inhibitor of the Interaction between β-Catenin and CBP, Exerts Antitumor Activity in Tumor Models with Activated Canonical Wnt Signaling

[4] Kevin Brown Chandler, et al. Mol Omics. β-Catenin/CBP inhibition alters epidermal growth factor receptor fucosylation status in oral squamous cell carcinoma

[5] Masaru Katoh. Int J Mol Med. Multi‑layered prevention and treatment of chronic inflammation, organ fibrosis and cancer associated with canonical WNT/β‑catenin signaling activation (Review)

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Keywords: E7386 supplier, Epigenetic Reader Domain, inhibitors, activators


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