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首页-抗体药物偶连体和PROTACs-PROTAC-MRT-2359
MRT-2359

Chemical Structure : MRT-2359

CAS No.: 2803881-11-8

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MRT-2359 (MRT 2359, MRT2359)

货号: 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%).

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5 mg ￥3580 In stock
10 mg ￥5580 In stock
25 mg ￥8980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 495.39
分子式 C22H17F4N3O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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

参考文献

1. Gerald Gavory, et al. Cancer Res (2022) 82 (12_Supplement): 3929.

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