NT219

NT219 is a potent and dual inhibitor of insulin receptor substrates 1/2 (IRS1/2) and STAT3. IRS1/2 and STAT3 are major signaling junctions regulated by various oncogenes. NT219 affects IRS1/2 degradation and inhibits STAT3 phosphorylation. NT219 has the potential for the research of cancer diseases[1].

Product Specifications

CAS Number

[1198078-60-2]

UNSPSC

12352005

Target

Insulin Receptor; STAT

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/nt219.html

Purity

98.57

Solubility

DMSO : ≥ 100 mg/mL

Smiles

OC(C=C1CNC(/C=C/C2=C(C(O)=C(C=C2)O)Br)=S)=C(C(O)=C1)O

Molecular Formula

C16H14BrNO5S

Molecular Weight

412.26

References & Citations

[1]Alberto Bessudo, et al. A phase 1/2 study with open-label, dose escalation phase followed by single-arm expansion at the maximum tolerated dose to assess the safety, tolerability, pharmacokinetics, pharmacodynamics, and efficacy of NT219 injection alone and in combination with cetuximab in adults with advanced solid tumors and head and neck cancer.|[2]Reuveni H, et al. NT219, a dual inhibitor of IRS1/2 and STAT3, suppresses cancer stem cell-mediated resistance to KRASG12C and KRASG12D inhibitors in solid tumors[J]. cell, 2024, 3 (2) : 1.|[3]Reuveni H, et al. NT219, a novel dual inhibitor of STAT3 and IRS1/2, demonstrates anti-tumor activity with and without cetuximab in pembrolizumab-resistant head and neck cancer PDX models[C]//Cancer Research. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2020, 80 (16) .