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Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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SKU | Size | Availability | Price | Qty |
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E648443-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $500.90 | |
E648443-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $850.90 | |
E648443-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,800.90 | |
E648443-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $3,000.90 | |
E648443-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $4,600.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | E64FC26 is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC 50 s 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. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | E64FC26 is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC 50 s 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. In Vitro E64FC26 (0.01-100 μM; 24 hours) shows anti-MM activity , with an EC 50 of 0.59 μM.?\nE64FC26 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MM.1S BzR cells Concentration: 0.01, 0.1, 1, 10, 100 µM Incubation Time: 24 hours Result: Showed anti-MM activity , with an EC 50 of 0.59 μM. 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 . ?\nThe combination of E64FC26 and Bortezomib produced the greatest improvement in survival, extending the median survival by 20 days . ?\nPharmacokinetic 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 (C max ) of 400 nM after a single oral dose of 5 mg/kg with a terminal half-life of 9.5 h . ?\nVk*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% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD-SCID IL2Rγ-/- (NSG) mice (bearing MM.1S cells) Dosage: 2 mg/ kg Administration: i.p.; three days a week for 7days Result: Showed a clear anti-MM effect in this model also, increasing median survival by 2 weeks. Form:Solid |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (1E)-1-nonylidene-3-(trifluoromethyl)indene-5,6-diol |
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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+ |
InChi Key | OWYMWLCFHDHVAH-UKTHLTGXSA-N |
Canonical SMILES | CCCCCCCCC=C1C=C(C2=CC(=C(C=C21)O)O)C(F)(F)F |
Isomeric SMILES | CCCCCCCC/C=C/1\C=C(C2=CC(=C(C=C21)O)O)C(F)(F)F |
PubChem CID | 137796284 |
Molecular Weight | 340.38 |
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Solubility | DMSO : 100 mg/mL (293.79 mM; Need ultrasonic) |
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