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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H361Suspected of damaging fertility or the unborn child
H373May cause damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P308+P313IF exposed or concerned: Get medical advice/attention.
P405Store locked up.
P501Dispose of contents/container to..…
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
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- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
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- +86-21-52996696
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- 021-65675885
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- QQ:2853530913
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- 021-QQ：65489617 15618227136
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- 21-5161 9052
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- 13504435624
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- 15317229551
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- 15151849396@163.com
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