Биологическая активность
IACS-13909 is a specific and мощный allosteric ингибитор of SHP2 that suppresses the signaling of RTK/MAPK pathway and overcomes multiple mechanisms underlying osimertinib resistance. IACS-13909 potently impedes the proliferation of tumors with a broad spectrum of RTKs as the oncogenic driver. Importantly, in NSCLC models with acquired resistance to osimertinib, IACS-13909 administered as a single agent or in combination with osimertinib potently reduces tumor клетка proliferation in vitro and in vivo. Together, our findings provide preclinical evidence for using a SHP2 ингибитор as a therapeutic strategy in acquired EGFR ингибитор-resistant NSCLC.
Оригинал на английском
IACS-13909 is a specific and potent allosteric inhibitor of SHP2 that suppresses the signaling of RTK/MAPK pathway and overcomes multiple mechanisms underlying osimertinib resistance. IACS-13909 potently impedes the proliferation of tumors with a broad spectrum of RTKs as the oncogenic driver. Importantly, in NSCLC models with acquired resistance to osimertinib, IACS-13909 administered as a single agent or in combination with osimertinib potently reduces tumor cell proliferation in vitro and in vivo. Together, our findings provide preclinical evidence for using a SHP2 inhibitor as a therapeutic strategy in acquired EGFR inhibitor-resistant NSCLC.
Химические свойства
- CAS №
- 2160546-07-4
- Брутто-формула
- C₁₇H₁₈Cl₂N₆
- Мол. масса
- 377.27 г/моль
- SMILES
- ClC1C(Cl)=C(C2C3N=CC(=NC=3NN=2)N2CCC(N)(C)CC2)C=CC=1
- Синонимы
- IACS-13909; IACS 13909; IACS13909
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели4°C в ДМСО,6 мес.-80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.