2446965-01-9
Chemical Structure
JR4-187
- CAS No.: 2446965-01-9
- Formula:C23H25FN6O2
- Molecular Weight:436.48
InChIKey: YLACLZPNGQXHKG-LHSJRXKWSA-N
SMILES: O=C(NC1=C2N=CC=CC2=CC(F)=C1)C3=CN=C(N(CC4)CCC4([C@@H]5N)CO[C@H]5C)C=N3
Biological Activity: JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein. JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer[1][2].
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JR4-187 | JR4-187 is an orally active, copper-dependent anticancer agent. JR4-187 downregulates genes involved in oxidative phosphorylation, MYC targets and E2F targets in cancer cells, while upregulates genes involved in the TNF-α signaling pathway, p53 pathway and KRAS signaling pathway, and downregulates CTR1 protein. JR4-187 induces ROS production, apoptosis, copper-dependent cytotoxicity, and exhibits selective cytotoxicity against KRAS-mutant cancer cells. JR4-187 is well tolerated in mouse models of pancreatic cancer. JR4-187 can be used in research related to cancers such as pancreatic ductal adenocarcinoma, colon cancer and rectal cancer. | |||||||||||||||||||||
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References
- [1]. Rima Mouawad, et al. Copper Transporter 1-Mediated Deregulation of Copper Homeostasis Impacts MYC and Oxidative Phosphorylation Pathways and Increases the Sensitivity of Tumor Cells to Complex I Inhibitors.
- [2]. Roy J, et al. Copper-KRAS-COX2 Axis: A Therapeutic Vulnerability in Pancreatic Cancer. J Med Chem. 2025;68(8):8400-8428. [Content Brief]
