| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:E64FC26;E64FC26,E-64FC26
CAS:2285446-62-8
Purity:98% Package:10 mg;100 mg;25 mg;50 mg
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| Company Name: |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
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| Tel: |
021-59167510 18117107507 |
| Email: |
vip@med-life.cn |
| Products Intro: |
Product Name:E64FC26
CAS:2285446-62-8
Purity:>=99% Package:200mg;50mg;25mg;500mg;10mM*1mLinDMSO;10mg;5mg;100mg
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| | E64FC26 Basic information |
| Product Name: | E64FC26 | | Synonyms: | E64FC26;E64FC26,E-64FC26;1H-Indene-5,6-diol, 1-nonylidene-3-(trifluoromethyl)-, (1E)- | | CAS: | 2285446-62-8 | | MF: | C19H23F3O2 | | MW: | 340.38 | | EINECS: | | | Product Categories: | | | Mol File: | 2285446-62-8.mol |  |
| | E64FC26 Chemical Properties |
| Boiling point | 423.0±45.0 °C(Predicted) | | density | 1.249±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (293.79 mM; Need ultrasonic) | | pka | 9.34±0.20(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | E64FC26 Usage And Synthesis |
| 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 |
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