2. Cell Cycle/DNA Damage Apoptosis
  3. Eukaryotic Initiation Factor (eIF) Apoptosis
  4. CR-1-31-B

CR-1-31-B is a synthetic rocaglate and a potent eIF4A inhibitor. CR-1-31-B exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis. CR-1-31-B perturbs association of Plasmodium falciparum eIF4A (PfeIF4A) with RNA. CR-1-31-B induces apoptosis of neuroblastoma and gallbladder cancer cells.

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CR-1-31-B Chemical Structure

CR-1-31-B Chemical Structure

CAS No. : 1352914-52-3

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10 mg USD 1180 In-stock
25 mg USD 2100 In-stock
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Based on 5 publication(s) in Google Scholar

CR-1-31-B Related Antibodies

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Description

CR-1-31-B is a synthetic rocaglate and a potent eIF4A inhibitor. CR-1-31-B exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis. CR-1-31-B perturbs association of Plasmodium falciparum eIF4A (PfeIF4A) with RNA. CR-1-31-B induces apoptosis of neuroblastoma and gallbladder cancer cells[1][2][3][4].

IC50 & Target

eIF4

 

In Vitro

CR-1-31-B (100 nM; 24 hours) inhibits MUC1-C translation in MCF-10A cells (EGF-stimulated)[1].
CR-1-31-B (10 and 100 nM) decreases MUC1-C abundance in MDA-MB-468 breast cancer cells[1].
CR-1-31B sensitizes gallbladder cancer cells to TRAIL-mediated apoptosis through the translational downregulation of c-FLIP[2].
Neuroblastoma (NB) cell lines exhibit decreased viability, increased apoptosis rates as well as changes in cell cycle distribution when treated with the synthetic rocaglate CR-1-31-B (24-72 hours), which clamps eIF4A and eIF4F onto mRNA, resulting in a translational block[4].
CR-1-31-B (100 nM; 5 hours) treatment increases reverse glutamine metabolism in pancreatic cancer cells[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CR-1-31-B Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-10A cells (EGF-stimulated)
Concentration: 100 nM
Incubation Time: 24 hours
Result: Blocked increases in MUC1-C abundance.

Cell Viability Assay[4]

Cell Line: SH-SY5Y cells and Kelly cells
Concentration: 0.1-100 nM
Incubation Time: 24-72 hours
Result: A significant decrease in SH-SY5Y viability was observed at 10 nM for all time points. Significantly decreased 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 Line: SH-SY5Y and Kelly cells
Concentration: SH-SY5Y cells were treated with 10, 20, and 50 nM and Kelly cells with 1, 5, and 10 nM
Incubation Time: 24-72 hours
Result: Triggered apoptosis.
In Vivo

CR-1-31-B (2 mg/kg in 60 μL olive oil; IP; once every 2 days for 28 days) reduces the growth and initiates TRAIL-induced apoptosis in a BALB/c nude mice model of gallbladder cancer cells (GBC)[2].
CR-1-31-B (0.2 mg/kg; IP; daily for 7 days; murine orthotopic transplant model of pancreatic ductal adenocarcinoma) effectively inhibits protein synthesis and growth of pancreatic tumours[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

507.53

Formula

C28H29NO8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]([C@H]1C2=CC=CC=C2)[C@@H](O)[C@]3(O)[C@@]1(C4=CC=C(OC)C=C4)OC5=CC(OC)=CC(OC)=C35)NOC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 230 mg/mL (453.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5.75 mg/mL (11.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5.75 mg/mL (11.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.36%

COA (262 KB) LCMS (257 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9703 mL 9.8516 mL 19.7033 mL 49.2582 mL
5 mM 0.3941 mL 1.9703 mL 3.9407 mL 9.8516 mL
10 mM 0.1970 mL 0.9852 mL 1.9703 mL 4.9258 mL
15 mM 0.1314 mL 0.6568 mL 1.3136 mL 3.2839 mL
20 mM 0.0985 mL 0.4926 mL 0.9852 mL 2.4629 mL
25 mM 0.0788 mL 0.3941 mL 0.7881 mL 1.9703 mL
30 mM 0.0657 mL 0.3284 mL 0.6568 mL 1.6419 mL
40 mM 0.0493 mL 0.2463 mL 0.4926 mL 1.2315 mL
50 mM 0.0394 mL 0.1970 mL 0.3941 mL 0.9852 mL
60 mM 0.0328 mL 0.1642 mL 0.3284 mL 0.8210 mL
80 mM 0.0246 mL 0.1231 mL 0.2463 mL 0.6157 mL
100 mM 0.0197 mL 0.0985 mL 0.1970 mL 0.4926 mL
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CR-1-31-B Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CR-1-31-B1352914-52-3Eukaryotic Initiation Factor (eIF)ApoptosisMUC1-CneuroblastomatranslationabundancegrowthfactorstimulationbreastcancercellsMCF-10ApancreaticductaladenocarcinomaInhibitorinhibitorinhibit

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