7H-Thieno[3,2-b]pyran-7-one, 3-[4-[[4-[4-(1-azetidinylmethyl)-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]phenyl]-5-(4-morpholinyl)-

Biological Activity

SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression[1][2]. SRX3207 (10 μmol/L) is able to block p-AKT at concentration[1].SRX3207 has sufficient solubility in water (43 μmol/L)[1]. SRX3207 (10 mg/kg, orally) increases antitumor immune response[1].

References

[1]. Shweta Joshi, et al. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Molecular Cancer Therapeutics. 2020. [2]. Shweta Joshi, et al. Macrophage Syk-PI3Kγ Inhibits Antitumor Immunity: SRX3207, a Novel Dual Syk-PI3K Inhibitory Chemotype Relieves Tumor Immunosuppression. Mol Cancer Ther. 2020 Mar;19(3):755-764.