| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
E64FC26 has anti-MM action with an EC50 of 0.59 μM (0.01-100 μM; 24 hours) [1]. E64FC26 demonstrated notable cytotoxicity in genetically varied 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) [1].
|
|---|---|
| ln Vivo |
In an NSG mouse model, intraperitoneal administration of E64FC26 (2 mg/kg; three days per week for seven days) demonstrated anti-MM effects, extending the median survival by 2 weeks [1]. The two treatments that increased survival the most were bortezomib and E64FC26, which extended median survival by 20 days [1]. In CD-1 mice, the pharmacokinetics of E64FC26 were assessed. The intravenous administration of E64FC26 (2 mg/kg; gray trace) or side-study (5 mg/kg; blue trace) resulted in the measurement of drug concentrations during a 24-hour period. A single mouse dose of 5 mg/kg resulted in systemic exposure that reached a maximum concentration (Cmax) of 400 nM with a terminal half-phase decline of 9.5 hours, indicating sufficient local bioavailability in CD-1 mice. 34% [1]. Scenario mode Vk*MYC E64FC26 is continuously administered during the day (2 mg/kg, intraperitoneal injection, 3 days/week). In all mice, E64FC26 can cause an instant anti-MM reaction and reduce serum M protein by 33 ± 7.9% on average [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: MM. 1S BzR Cell Tested Concentrations: 0.01, 0.1, 1, 10, 100 µM Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated anti-MM activity with EC50 of 0.59 µM. |
| Animal Protocol |
Animal/Disease Models: NOD-SCID IL2Rγ-/- (NSG) mice (carrying MM.1S cells) [1]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip) injection; three days per week for 7 days Experimental Results: here The model also demonstrated significant anti-MM effects, extending median survival by 2 weeks. |
| References |
| Molecular Formula |
C19H23F3O2
|
|---|---|
| Molecular Weight |
340.37993645668
|
| Exact Mass |
340.165
|
| CAS # |
2285446-62-8
|
| Related CAS # |
(E/Z)-E64FC26;2285446-67-3
|
| PubChem CID |
137796284
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
6.5
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
24
|
| Complexity |
468
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC(C1=C/C(=C\CCCCCCCC)/C2C=C(C(=CC=21)O)O)(F)F
|
| InChi Key |
OWYMWLCFHDHVAH-UKTHLTGXSA-N
|
| InChi Code |
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+
|
| Chemical Name |
(1E)-1-nonylidene-3-(trifluoromethyl)indene-5,6-diol
|
| Synonyms |
E64-FC26; E64 FC26
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~293.79 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL | |
| 5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL | |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9379 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
