| Hazard Information | Back Directory | [Uses]
PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity[1]. PI3Kγ inhibitor 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
PI3Kγ inhibitor 7 (compound 2) (5 mg/kg; p.o.) shows good pharmacokinetic absorption with t1/2 of 3.4 h, F of 60 % in ICR mice[1].
PI3Kγ inhibitor 7 (60 mg/kg; p.o.; daily for 21 days) shows antitumor activity in mice[1]. | Animal Model: | Female BALB/c mice (CT26 cells)[1] | | Dosage: | 60 mg/kg | | Administration: | P.o.; daily for 21 days | | Result: | Decreased the tumor weight and with TGI of 51.2%, IR of 52.1%. |
| [IC 50]
PI3Kα: 4768 nM (IC50); PI3Kβ: 878.1 nM (IC50); PI3Kγ: 3.42 nM (IC50); PI3Kδ: 355.2 nM (IC50) | [References]
[1] HeJun Lv, et al. Alkyne derivative, preparation method for same, and uses thereof. WO2021004421A1. |
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