Vulolisib (C09-1184-852)

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 ). Specifications and Purity: 99%. Molecular Formula: C18H19F2N5O3S. Molecular Weight: 423.44. PubChem CID: 146267141. Isomeric SMILES: C[C@@H](C(=O)N)NC1=CC2=C(C=C1)C3=NC(=CN3CCO2)N4[C@@H](CSC4=O)C(F)F.