E64FC26

E64FC26 is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6, respectively. E64FC26 shows anti-myeloma activity.

Product information

CAS Number: 2285446-62-8

Molecular Weight: 340.38

Formula: C19H23F3O2

Chemical Name: (1E)-1-nonylidene-3-(trifluoromethyl)-1H-indene-5,6-diol

Smiles: CCCCCCCC/C=C1\C=C(C2=CC(O)=C(O)C=C2\1)C(F)(F)F

InChiKey: OWYMWLCFHDHVAH-UKTHLTGXSA-N

InChi: InChI=1S/C19H23F3O2/c1-2-3-4-5-6-7-8-9-13-10-16(19(20,21)22)15-12-18(24)17(23)11-14(13)15/h9-12,23-24H,2-8H2,1H3/b13-9+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (293.79 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

E64FC26 (0.01-100 µM; 24 hours) shows anti-MM activity , with an EC50 of 0.59 μM.E64FC26 is more cytotoxic against a genetically diverse panel of multiple myeloma (MM) cell lines (KMS11, OPM2, MM.1S BzR, MM.1S, SA-13, U266 BzR, ANBL6, KMS12PE, U266, 8226 DxR, 8226 BzR, KMS12BM, H929,8226 cells) when compared to non-malignant cells.

In Vivo:

E64FC26 (2 mg/ kg; i.p.; three days a week for 7days) shows anti-MM effect in NSG mice model, and increases median survival by 2 weeks. The combination of E64FC26 and Bortezomib produced the greatest improvement in survival, extending the median survival by 20 days. Pharmacokinetic of E64FC26 was measured in CD-1 mice. E64FC26 was administered i.v. (2 mg/kg; gray tracing) or p.o. (5 mg/ kg; blue tracing) and plasma drug concentrations were measured over a 24 h period. In CD-1 mice demonstrated adequate oral bioavailabilty of 34% with systemic exposure approaching a maximum concentration (Cmax) of 400 nM after a single oral dose of 5 mg/kg with a terminal half-life of 9.5 h. Vk*MYC transgenic mice are treated with E64FC26 (2 mg/kg, i.p., 3 days/week) for two consecutive weeks. E64FC26 treatment induces an immediate anti-MM response, decreasing serum M-protein in all mice by an average of 33 ± 7.9%.

Products are for research use only. Not for human use.