IACS-13909 是具有口服活性的、选择性的SHP2变构抑制剂，其IC50=15.7 nM，Kd=32 nM。与其他磷酸酶相比，它对SHP2的选择性更高。它能够抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导，并具有抗癌作用。

IACS-13909, a specific and potent allosteric inhibitor of SHP2, that suppresses signaling through the MAPK pathway.

IACS-13909 potently impeded proliferation of tumors harboring a broad spectrum of activated RTKs as the oncogenic driver.

In EGFR-mutant osimertinib-resistant NSCLC models with EGFR-dependent and EGFR-independent resistance mechanisms, IACS-13909, administered as a single agent or in combination with osimertinib, potently suppressed tumor cell proliferation?in vitro?and caused tumor regression?in vivo.

2160546-07-4

C17H18Cl2N6

377.27

DMSO:9 mg/mL (23.86 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years