MedChemExpress LLC (MCE)

MedChemExpressModel MRT-2359 - 2803881-11-8

SHARE
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].
Most popular related searches

MCE products for research use only. We do not sell to patients.

MRT-2359

MCE China:MRT-2359

Brand:MedChemExpress (MCE)

Cat. No.HY-153356

CAS:2803881-11-8

Purity:99.91%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and 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.

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].

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].

IC50 & Target:IC50: >30 nM and [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. 0 --> MRT-2359 Related Antibodies

Hot selling product:Hyaluronidase  | G15  | Pemigatinib  | (S)-Mephenytoin  | Proteinase K  | Sulfasalazine  | Aspirin  | PKM2-IN-1  | Auranofin  | Indomethacin

Trending products:Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References:

[1]. Gavory G, et al. Development of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for the treatment of lung cancers with MYC-induced translational addiction[J]. Cancer Research, 2023, 83(7_Supplement): 3449-3449.

[2]. Fasching Bernhard, et al. Preparation of isoindolinone compounds as modulators of cereblon. Patent. WO2022152821.

[3]. Gerald Gavory, et al. Abstract 3929: Identification of MRT-2359 a potent, selective and orally bioavailable GSPT1-directed molecular glue degrader (MGD) for the treatment of cancers with Myc-induced translational addiction. Cancer Res 15 June 2022; 82 (12_Supplement): 3929.

[4]. Gerald Gavory, et al. Abstract 3449: Development of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for the treatment of lung cancers with MYC-induced translational addiction. Cancer Res 1 April 2023; 83 (7_Supplement): 3449.

[5]. Ralph Tiedt, et al. Abstract 3294: The GSPT1 molecular glue degrader MRT-2359 is active against prostate cancer. Cancer Res 15 March 2024; 84 (6_Supplement): 3294

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
•   It has a professional experimental center and strict quality control and verification system;
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
•   The biological activity of the products has been verified by the experiments of customers in various countries;
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。