| Description |
AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
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Targets
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| PI3Kδ [1] |
PI3Kγ [1] |
PI3Kβ [1] |
PI3Kα [1] |
| 18 nM |
850 nM |
2.7μM |
33 μM |
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| In vitro |
AMG319 inhibits anti-IgM/CD40L-induced B cell proliferation with IC50 of 8.6 nM and reduces pAkt level with IC50 of 1.5 nM. AMG319 also inhibits anti-IgD-induce CD-69 expression in HWB. [1]
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| In vivo |
In female Lewis rats, AMG319 (3 mg/kg, p.o.) inhibits the KLH-induced inflammatory response by 88%. In the transgenic (IgMm) mice, AMG319 (, p.o.) inhibits in vivo pAKT with IC50 of 1.9 nM. [1]
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COA
HPLC