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[1][2][3][4].

Product Specifications

CAS Number

[2070837-24-8]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Autophagy; CDK; FGFR; PI3K; Reactive Oxygen Species (ROS)

Related Pathways

Autophagy; Cell Cycle/DNA Damage; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

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

Molecular Formula

C25H29Cl3N8O3

Molecular Weight

595.91

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[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.|[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.|[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.|[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.