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Chemical Structure : MRT-2359
CAS No.: 2803881-11-8
Catalog No.: PC-20680Not For Human Use, Lab Use Only.
MRT-2359 (MRT2359) is a potent, selective and orally bioavailable GSPT1-directed molecular glue degrader with DC50 of 5 nM in CAL51 cell line (Dmax=100%).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $558 | In stock | |
| 25 mg | $898 | In stock | |
| 100 mg | Get quote | ||
| 200 mg | Get quote |
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MRT-2359 (MRT2359) is a potent, selective and orally bioavailable GSPT1-directed molecular glue degrader with DC50 of 5 nM in CAL51 cell line (Dmax=100%).
MRT-2359 potently inhibits cell viability in CAL51 cancer cell line with EC50 of 150 nM.
MRT-2359 induces the degradation of GSPT1, the associated downregulation of N-MYC and the modulation of its transcriptional output leading to preferential anti-proliferative activity in L-MYC and N-MYC driven cancer cells.
MRT-2359 administered orally demonstrates preferential anti-tumor activity in xenograft and PDX NSCLC models with high L-MYC and/or N-MYC mRNA expression levels.
MRT-2359 promotes complex formation between CRBN and GSPT1 and potently induces GSPT1 degradation in a CRBN- and degron-dependent manner.
MRT-2359 degrades GSPT1 in a large panel of cancer lines revealed profound and preferential antiproliferative activity in Myc-driven cell lines, such as high N-Myc expressing non-small cell lung cancer (NSCLC) lines and high L-Myc expressing small cell lung cancer (SCLC) lines.
| M.Wt | 495.39 | |
| Formula | C22H17F4N3O6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
O=C(NC1=CC(OC(F)(F)F)=CC=C1F)OCC2=CC=C3C(C(N(C4C(NC(CC4)=O)=O)C3)=O)=C2 |
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1. Gerald Gavory, et al. Cancer Res (2022) 82 (12_Supplement): 3929.
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