2070837-24-8
Chemical Structure
MPT0L145
- CAS No.: 2070837-24-8
- Formula:C25H29Cl3N8O3
- Molecular Weight:595.91
IUPAC Name: 1-(4-((4-(4-ethylpiperazin-1-yl)phenyl)amino)-1,3,5-triazin-2-yl)-1-methyl-3-(2,4,6-trichloro-3,5-dimethoxyphenyl)urea
InChIKey: XXXJOFNWFFKBRC-UHFFFAOYSA-N
SMILES: O=C(NC1=C(Cl)C(OC)=C(Cl)C(OC)=C1Cl)N(C2=NC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=NC=N2)C
Biological Activity: MPT0L145 is a PIK3C3/FGFR inhibitor, with a Kd value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC[1][2][3][4].
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MPT0L145 | MPT0L145 is a PIK3C3/FGFR inhibitor, with a Kd value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC. | |||||||||||||||||||||
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- [1]. Chen CH, et al. Targeting Autophagy by MPT0L145, a Highly Potent PIK3C3 Inhibitor, Provides Synergistic Interaction to Targeted or Chemotherapeutic Agents in Cancer Cells. Cancers (Basel). 2019 Sep 11;11(9):1345. [Content Brief]
- [2]. Chen CH, et al. Trichlorobenzene-substituted azaaryl compounds as novel FGFR inhibitors exhibiting potent antitumor activity in bladder cancer cells in vitro and in vivo. Oncotarget. 2016 May 3;7(18):26374-87. [Content Brief]
- [3]. Hsieh TH, et al. Combining an Autophagy Inhibitor, MPT0L145, with Abemaciclib Is a New Therapeutic Strategy in GBM Treatment. Cancers (Basel). 2021 Dec 4;13(23):6117. [Content Brief]
- [4]. Chen CH, et al. Dual Inhibition of PIK3C3 and FGFR as a New Therapeutic Approach to Treat Bladder Cancer. Clin Cancer Res. 2018 Mar 1;24(5):1176-1189. [Content Brief]
Keywords
