Description
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC 50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activityIn VitroVulolisib has antiproliferative activity against PI3Kα-mutant cell lines HCC1954 (H1047R), HGC-27 (E542K) and MKN1 (E545K) with IC 50 s of 21 nM, 60 nM and 40 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoVulolisib (10, 30 and 60 mg/kg; IG; daily for 7days) exhibits better tolerance and exposure than Inavolisib. Vulolisib (10mg/kg; PO; daily for 19 days) inhibits tumor growth with TGI of 132%. Vulolisib (5 mg/kg; IG, single dosage) exhibits favorable pharmacokinetic property. Pharmacokinetic Parameters of Vulolisib in male Balb/c mice. IG (5 mg/kg) t max (h) 0.5 C max (ng/mL) 1057 AUC 0-t (ng/mL·h) 2185 AUC 0-∞ (ng/mL·h) 2274 t 1/2 (h) 1.6 MRT (h) 2.2 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats Dosage: 10, 30 and 60 mg/kg Administration: IG; daily for 7days Result: Exhibited better tolerance and exposure than Inavolisib. Animal Model: Female BALB/c nude mice (6-8 weeks; injected with HCC1954) Dosage: 10mg/kg Administration: PO; daily for 19 days Result: Inhibited tumor growth with TGI of 132%. Animal Model: Male Balb/c mice Dosage: 5 mg/kg Administration: IG, single dosage (Pharmacokinetic Analysis) Result: Exhibited favorable pharmacokinetic property.Form:SolidIC50& Target:PI3Kα 0.2 nM (IC 50 ) PI3Kβ 168 nM (IC 50 ) PI3Kγ 90 nM (IC 50 ) PI3Kδ 49 nM (IC 50 )