MRT-2359
- Product Name
- MRT-2359
- CAS No.
- 2803881-11-8
- Chemical Name
- MRT-2359
- Synonyms
- MRT-2539;MRT-2359;MRTX2359;MRT-2359, 10 mM in DMSO;2-(2,6-Dioxo-3-piperidyl)-3-oxo-5-isoindolinyl]methyl [2-Fluoro-5-(trifluoromethoxy)phenyl]carbamate;(2-(2,6-dioxopiperidin-3-yl)-3-oxoisoindolin-5-yl)methyl (2-fluoro-5-(trifluoromethoxy)phenyl)carbamate;[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-3-oxo-1H-isoindol-5-yl]methyl N-[2-fluoro-5-(trifluoromethoxy)phenyl]carbamate
- CBNumber
- CB813359698
- Molecular Formula
- C22H17F4N3O6
- Formula Weight
- 495.38
- MOL File
- 2803881-11-8.mol
MRT-2359 Property
- Boiling point:
- 644.0±55.0 °C(Predicted)
- Density
- 1.548±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
- pka
- 10.68±0.40(Predicted)
- form
- Solid
- color
- White to off-white
- InChIKey
- HNTGMIGBGVFOBT-UHFFFAOYSA-N
- SMILES
- C(OCC1C=CC2=C(C=1)C(=O)N(C1CCC(=O)NC1=O)C2)(=O)NC1=CC(OC(F)(F)F)=CC=C1F
MRT-2359 Chemical Properties,Usage,Production
Uses
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].
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].
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
MRT-2359 Preparation Products And Raw materials
Raw materials
Preparation Products
MRT-2359 Suppliers
- Tel
- 18014399201
- sales@chemlab-tachizaki.com
- Country
- China
- ProdList
- 2755
- Advantage
- 58
- Tel
- 13771642864
- Fax
- 1078336263
- snhuyu_2008@126.com
- Country
- China
- ProdList
- 1171
- Advantage
- 58
- Tel
- 18149758185 18149758185;
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3505
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4800
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9803
- Advantage
- 58
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9531
- Advantage
- 58
- Tel
- 13504435624
- 1927928688@qq.com
- Country
- China
- ProdList
- 1623
- Advantage
- 58
- Tel
- 020-82000279 18988941452
- Fax
- QQ：3283937693
- YN_research@163.com
- Country
- China
- ProdList
- 3000
- Advantage
- 58
- Tel
- 15317229551
- Fax
- QQ:3607245178
- 15151849396@163.com
- Country
- China
- ProdList
- 989
- Advantage
- 58
- Tel
- 15865264761
- 486064515@qq.com
- Country
- China
- ProdList
- 4858
- Advantage
- 58