E64FC26

SKU: orb1709807

Description

E64FC26 is a pan-inhibitor of the protein disulfide isomerase (PDI) family, targeting members including PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6. It exhibits antitumor activity and is a useful research tool for studying cancers such as multiple myeloma and pancreatic cancer in both in vitro and in vivo models.

Research Area

Cell Biology

Key Properties

• CAS Number: 2285446-62-8
• MW: 340.38
• Purity: 98.10% (May vary between batches)
• Formula: C₁₉H₂₃F₃O₂
• SMILES: C(F)(F)(F)C=1C=2C(\C(=C\CCCCCCCC)\C1)=CC(O)=C(O)C2
• Target: Apoptosis,Others
• Solubility: 10% DMSO+90% Saline:3.3 mg/mL (9.7 mM);DMSO:80 mg/mL (235.03 mM)

Bioactivity

• Target IC50:
  anti-multiple myeloma:0.59 μM (EC50)
• In Vivo:
  In the NSG mouse model, E64FC26 (2 mg/kg; intraperitoneal injection; three times a week for 7 days) demonstrates anti-multiple myeloma (MM) effects, extending the median survival by 2 weeks. The maximum improvement in median survival is observed with both E64FC26 and Bortezomib, leading to a 20-day extension in median survival.The pharmacokinetics of E64FC26 were measured in CD-1 mice. E64FC26 was administered via intravenous injection (2 mg/kg; gray trace) or oral administration (5 mg/kg; blue trace), and plasma drug concentrations were measured within 24 hours. In CD-1 mice, after a single oral dose of 5 mg/kg, the maximum concentration (Cmax) reached 400 nM with a terminal half-life of 9.5 hours, demonstrating sufficient oral bioavailability of 34%. Vk*MYC transgenic mice were treated with E64FC26 (2 mg/kg, intraperitoneal injection, 3 days/week) for two consecutive weeks. E64FC26 treatment induces an immediate anti-MM response, resulting in an average reduction of 33 ± 7.9% in serum M protein for all mice.
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• In Vitro:
  E64FC26 exhibits anti-multiple myeloma (MM) activity with an EC50 of 0.59 μM after 24 hours of treatment in a concentration range of 0.01-100 μM. E64FC26 demonstrates significant cytotoxicity in a panel of genetically diverse multiple myeloma cell lines (KMS11, OPM2, MM.1S BzR, MM.1S, SA-13, U266 BzR, ANBL6, KMS12PE, U266, 8226 DxR, 8226 BzR, KMS12BM, H929, 8226 cells).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E64FC26, E-64FC26, protein disulfide isomerase (PDI)

Compound Identifiers

PubChem CID

137796284