E64FC26
- CAS No.
- 2285446-62-8
- Chemical Name:
- E64FC26
- Synonyms
- E64FC26;E64FC26,E-64FC26;1H-Indene-5,6-diol, 1-nonylidene-3-(trifluoromethyl)-, (1E)-
- CBNumber:
- CB08054386
- Molecular Formula:
- C19H23F3O2
- Molecular Weight:
- 340.38
- MDL Number:
- MFCD32858273
- MOL File:
- 2285446-62-8.mol
E64FC26 Chemical Properties,Uses,Production
Biological Activity
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[1]. E64FC26 (0.01-100 μM; 24 hours) shows anti-MM activity , with an EC50 of 0.59 μM[1].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[1]. 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[1].The combination of E64FC26 and Bortezomib produced the greatest improvement in survival, extending the median survival by 20 days[1].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[1].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%[1].
References
[1]. Robinson RM, et al. Inhibitors of the protein disulfide isomerase family for the treatment of multiple myeloma. Leukemia. 2019 Apr;33(4):1011-1022.
E64FC26 Preparation Products And Raw materials
Raw materials
Preparation Products
E64FC26 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 23963 | 58 |
| Shanghai Yiyan Biotechnology Co. , Ltd. | 021-69985186 13611928337 | 3427709316@qq.com | China | 7980 | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 5012 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9268 | 58 |