IACS-13909 |
| Catalog No.GC62345 |
IACS-13909 est un inhibiteur allostérique SHP2 sélectif, puissant et actif par voie orale avec une IC50 de 15,7 nM et un Kd de 32 nM. IACS-13909 est plus sélectif pour SHP2 que les autres phosphatases (y compris SHP1). IACS-13909 a des activités antitumorales et supprime la signalisation de la voie MAPK dans les cancers dépendants des récepteurs tyrosine kinases (RTK).
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Cas No.: 2160546-07-4
Sample solution is provided at 25 µL, 10mM.
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IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd 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[1].
IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells[1].IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells[1].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[1].
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[1].
[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.
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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