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].

NT219 (5 μM, 8 or 12 days) suppresses cancer stem cell viability as monotherapy and synergizes with sotorasib to induce disintegration of established mKRAS (G12C) NSCLC spheroids^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NT219 (20 or 60 mg/kg, i.v., twice a week for 24 days) inhibited tumor cell growth and enhanced the anti-cancer effects of Cetuximab (HY-P9905) and Pembrolizumab (HY-P9902) in the SCC-9 cell xenograft model of recurrent and metastatic head and neck squamous cell carcinoma (NOD scid gamma mice)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

412.26

C₁₆H₁₄BrNO₅S

1198078-60-2

Solid

Yellow to brown

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

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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).