2. Apoptosis
  3. Apoptosis
  4. MRT-2359

MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research.

For research use only. We do not sell to patients.

MRT-2359 Chemical Structure

MRT-2359 Chemical Structure

CAS No. : 2803881-11-8

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Based on 1 publication(s) in Google Scholar

MRT-2359 Related Antibodies

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  • Purity & Documentation

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Description

MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research[1][2][3][4][5].

IC50 & Target

IC50: >30 nM and <300 nM (HIV-1) [1]
In Vitro

MRT-2359 demonstrates significant selective activity in MYC-driven lung cancer. In a broad range of cancer cell lines, MRT-2359 exhibits pronounced and preferential anti-proliferative activity towards those cell lines with high N-Myc or L-Myc expression, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cell lines. However, MRT-2359 shows minimal to no effect on cell lines with low N-Myc or L-Myc expression[4].

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

MRT-2359 Related Antibodies
In Vivo

MRT-2359 completely degrades GSPT1 in high N-MYC non-small cell lung cancer (NSCLC) transplanted tumors and PDX models, reduces the expression level of N-Myc protein, consequently leading to a reduction in tumor size[3].
MRT-2359 (10 mg/kg; Oral gavage (p.o.); 5 days on, 9 days off, 4 weeks) can completely regress tumors in immunocompromised xenografted mouse models of AR-V7-positive cell lines 22RV1 and NCI-H660[5].

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

495.38

Formula

C22H17F4N3O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(OC(F)(F)F)=CC=C1F)OCC2=CC=C3C(C(N(C4C(NC(CC4)=O)=O)C3)=O)=C2
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 : 100 mg/mL (201.87 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 2.0187 mL 10.0933 mL 20.1865 mL
5 mM 0.4037 mL 2.0187 mL 4.0373 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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: 99.98%

COA (245 KB) HNMR (127 KB) RP-HPLC (138 KB) LCMS (231 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 2.0187 mL 10.0933 mL 20.1865 mL 50.4663 mL
5 mM 0.4037 mL 2.0187 mL 4.0373 mL 10.0933 mL
10 mM 0.2019 mL 1.0093 mL 2.0187 mL 5.0466 mL
15 mM 0.1346 mL 0.6729 mL 1.3458 mL 3.3644 mL
20 mM 0.1009 mL 0.5047 mL 1.0093 mL 2.5233 mL
25 mM 0.0807 mL 0.4037 mL 0.8075 mL 2.0187 mL
30 mM 0.0673 mL 0.3364 mL 0.6729 mL 1.6822 mL
40 mM 0.0505 mL 0.2523 mL 0.5047 mL 1.2617 mL
50 mM 0.0404 mL 0.2019 mL 0.4037 mL 1.0093 mL
60 mM 0.0336 mL 0.1682 mL 0.3364 mL 0.8411 mL
80 mM 0.0252 mL 0.1262 mL 0.2523 mL 0.6308 mL
100 mM 0.0202 mL 0.1009 mL 0.2019 mL 0.5047 mL
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MRT-2359 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:

MRT-23592803881-11-8MRT2359MRT 2359ApoptosisOrally activeAnti-tumor activityResistant non-small cell lung cancer cellsNSCLCSmall cell lung cancer cellsSCLC cellsMYC-driven cell linesPatient-derived xenograftsNeuroendocrine lung cancer PDXsInhibitorinhibitorinhibit

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