| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
eIF4
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|---|---|
| ln Vitro |
In MCF-10A cells (stimulated by EGF), CR-1-31-B (100 nM; 24 hours) suppresses MUC1-C translation [1]. MUC1-C abundance is decreased in MDA-MB-468 breast cancer cells by CR-1-31-B (10 and 100 nM) [1]. By translating down c-FLIP, CR-1-31B makes gallbladder cancer cells more susceptible to TRAIL-mediated apoptosis [2]. When treated with synthetic Rocaglate CR-1-31-B (24–72 hours), neuroblastoma (NB) cell lines show decreased viability, increased apoptosis rate, and changes in cell cycle distribution. A translational barrier is created when eIF4A and eIF4F are clamped onto mRNA [4]. In pancreatic cancer cells, treatment with CR-1-31-B (100 nM; 5 hours) enhances glutamine countermetabolism [5].
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| ln Vivo |
CR-1-31-B (2 mg/kg in 60 μL olive oil; i.p.; every 2 days for 28 days) in a BALB/c nude mouse model of gallbladder cancer cells Apoptosis of cells (GBC) inhibits growth and starts TRAIL induction[2]. Protein synthesis and pancreatic tumor growth are effectively inhibited by CR-1-31-B (0.2 mg/kg; intraperitoneal injection; once daily for 7 days; pancreatic ductal adenocarcinoma mouse orthotopic transplantation model) [5].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MCF-10A cells (EGF-stimulated) Tested Concentrations: 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Blocked increases in MUC1-C abundance. Cell Viability Assay[4] Cell Types: SH-SY5Y cells and Kelly cells Tested Concentrations: 0.1-100 nM Incubation Duration: 24-72 hrs (hours) Experimental Results: A significant decrease in SH -SY5Y viability was observed at 10 nM for all time points. Dramatically diminished the viability of Kelly cells at 5 nM. The calculated IC50 at 48 h was 20 nM for SH-SY5Y and 4 nM for Kelly cells. Apoptosis Analysis[4] Cell Types: SH-SY5Y and Kelly cells Tested Concentrations: SH-SY5Y cells were treated with 10, 20, and 50 nM and Kelly cells with 1, 5, and 10 nM Incubation Duration: 24-72 hrs (hours) Experimental Results: Triggered apoptosis. |
| References |
[1]. Jin C, Rajabi H, Rodrigo CM, Porco JA Jr, Kufe D. Targeting the eIF4A RNA helicase blocks translation of the MUC1-C oncoprotein. Oncogene. 2013;32(17):2179-2188.
[2]. Cao Y, et al. Targeting eIF4A using rocaglate CR 1 31B sensitizes gallbladder cancer cells to TRAIL mediated apoptosis through the translational downregulation of c FLIP. Oncol Rep. 2021;45(1):230-238. [3]. Langlais D, et al. Rocaglates as dual-targeting agents for experimental cerebral malaria. Proc Natl Acad Sci U S A. 2018;115(10):E2366-E2375. [4]. Skofler C, et al. Eukaryotic Translation Initiation Factor 4AI: A Potential Novel Target in Neuroblastoma. Cells. 2021;10(2):301. Published 2021 Feb 2. [5]. Chan K, et al. eIF4A supports an oncogenic translation program in pancreatic ductal adenocarcinoma. Nat Commun. 2019;10(1):5151. Published 2019 Nov 13. |
| Molecular Formula |
C28H29NO8
|
|---|---|
| Molecular Weight |
507.53
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| CAS # |
1352914-52-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O1C2C([H])=C(C([H])=C(C=2[C@@]2([C@@]([H])([C@]([H])(C(N([H])OC([H])([H])[H])=O)[C@@]([H])(C3C([H])=C([H])C([H])=C([H])C=3[H])[C@]12C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])O[H])O[H])OC([H])([H])[H])OC([H])([H])[H]
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : 230 mg/mL (453.18 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.75 mg/mL (11.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 57.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.75 mg/mL (11.33 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 57.5 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. View More
Solubility in Formulation 3: ≥ 5.75 mg/mL (11.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9703 mL | 9.8516 mL | 19.7033 mL | |
| 5 mM | 0.3941 mL | 1.9703 mL | 3.9407 mL | |
| 10 mM | 0.1970 mL | 0.9852 mL | 1.9703 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.
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