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首页-抗体药物偶连体和PROTACs-PROTAC-ZJK-807
ZJK-807

Chemical Structure : ZJK-807

CAS No.:

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ZJK-807 (ZJK807)

货号: PC-25610Not For Human Use, Lab Use Only.

ZJK-807 is a selective, cereblon (CRBN)-based proteolysis-targeting chimera (PROTAC) degrader of KRASG12D with DC50 of 79.5 nM in AsPC-1 cells (Dmax=92%), with minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D) KRAS proteins.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZJK-807 is a selective, cereblon (CRBN)-based proteolysis-targeting chimera (PROTAC) degrader of KRASG12D with DC50 of 79.5 nM in AsPC-1 cells (Dmax=92%), with minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D) KRAS proteins.
ZJK-807 combines an MRTX1133 analog with a VHL ligand, achieves efficient KRASG12D degradation.
ZJK-807 effectively reduces KRASG12D levels by 85 ± 2% at 1 μM and achieved an IC50 value of 0.22 uM in AsPC-1 cell line.
ZJK-807 is more effective in degrading KRASG12D in pancreatic cancer cells AsPC-1 compared to colorectal GP2D and gastric cancer cells AGS.
ZJK-807 exhibits antiproliferative effects on KRASG12D mutant cell lines, with IC50 values of 219.6 ± 43.8 nM in AsPC-1, 273.5 ± 58.9 nM in AGS, and 1110 ± 107.2 nM in GP2D cells, with no substantial antiproliferative activity in cell lines with wild-type or other KRAS mutations.
ZJK-807 has the potential to overcome acquired resistance to MRTX1133.
ZJK-807 (30 mg/kg, QD, SC) demonstrated in vivo antitumor efficiency in the AsPC-1 xenograft mice.

物理化学性质&存储条件

分子量 907.00
分子式 C50H48F2N10O5
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

5-(7-((1-(4-((1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl)-7-(8-ethynyl-7-fluoro-3-hydroxynaphthalen-1-yl)-8-fluoropyrido[4,3-d]pyrimidin-2-yl)azetidin-3-yl)(methyl)amino)-2-azaspiro[3.5]nonan-2-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

参考文献

1. Liu Z, et al. J Med Chem. 2025 Oct 9;68(19):20103-20129.

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