IACS-13909 是一种有效的选择性的，具有口服活性的 SHP2 变构抑制剂，其 IC₅₀ 为 15.7 nM，K_d 为 32 nM。与其他磷酸酶 (包括 SHP1) 相比，IACS-13909 对 SHP2 的选择性更高。IACS-13909 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 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC 50 of 15.7 nM and a K d of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.

Solid

IC50: 15.7 nM (SHP2)
Kd: 32 nM (SHP2)

IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells.
IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells.
IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Yuting Sun, et al. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853.

In Vitro: DMSO : 10 mg/mL (26.51 mM; Need ultrasonic)配制储备液