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首页-抗体药物偶连体和PROTACs-PROTAC-RP03707
RP03707

Chemical Structure : RP03707

CAS No.: 3030493-05-8

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RP03707

货号: PC-24575Not For Human Use, Lab Use Only.

RP03707 is a CRBN-involving, highly potent, and selective KRAS G12D PROTAC degrader with DC50 of 0.7 nM in PK-59 cells (Dmax=96%).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RP03707 is a CRBN-involving, highly potent, and selective KRAS G12D PROTAC degrader with DC50 of 0.7 nM in PK-59 cells (Dmax=96%).
RP03707 has a DC50 value of 0.6 nM for KRASG12D degradation, and pERK inhibition IC50 of 2.5 nM in AsPC-1 cells.
RP03707 exhibits no degradation activity against other RAS isoforms, including NRAS and HRAS, KRAS WT.
RP03707 also exhibits no degradation of IKZF1/3, in stark contrast to the positive control pomalidomide that showed expected IKZF1/3 depletion.
RP03707 exhibits a generally stronger antiproliferative effect against cancer cell lines carrying the KRASG12D mutant relative to MRTX1133.
RP03707 induces the degradation of both the active form and inactive forms of KRASG12D proteins concurrently in cells.
RP03707 (0.1-3 mg/kg, i.v.) exhibited significant antitumor effects with tumor growth inhibition (TGI >90%) in KRASG12D tumor-bearing mice.

物理化学性质&存储条件

分子量 994.14
分子式 C55H58F3N11O4
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

1-[6-[1-[7-[[1-[[4-(3,8-Diazabicyclo[3.2.1]octan-3-yl)-7-(8-ethynyl-7-fluoro-3-hydroxy-1-naphthyl)-8-fluoro-pyrido[4,3-d]pyrimidin-2-yl]oxymethyl]cyclopropyl]methyl]-7-azaspiro[3.5]nonan-2-yl]-4-piperidyl]-5-fluoro-1-methyl-indazol-3-yl]hexahydropyrimidine-2,4-dione

参考文献

1. Ji X, et al. J Med Chem. 2025 May 8. doi: 10.1021/acs.jmedchem.5c00428.

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