2390105-79-8

2390105-79-8 structure

Name: Vulolisib
Chemical Name: Vulolisib
CAS Number: 2390105-79-8
Molecular Formula: C₁₈H₁₉F₂N₅O₃S
Molecular Weight: 423.44
Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
Create Date: 2022-09-16 18:45:00
Modify Date: 2024-09-22 23:37:45
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity[1].

Name	Vulolisib

Description	Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Target	PI3Kα:0.2 nM (IC50) PI3Kβ:168 nM (IC50) PI3Kγ:90 nM (IC50) PI3Kδ:49 nM (IC50)
In Vitro	Vulolisib has antiproliferative activity against PI3Kα-mutant cell lines HCC1954 (H1047R), HGC-27 (E542K) and MKN1 (E545K) with IC50s of 21 nM, 60 nM and 40 nM, respectively[1].
In Vivo	Vulolisib (10, 30 and 60 mg/kg; IG; daily for 7days) exhibits better tolerance and exposure than Inavolisib[1]. Vulolisib (10mg/kg; PO; daily for 19 days) inhibits tumor growth with TGI of 132%[1]. Vulolisib (5 mg/kg; IG, single dosage) exhibits favorable pharmacokinetic property[1]. Pharmacokinetic Parameters of Vulolisib in male Balb/c mice[1]. IG (5 mg/kg) tmax (h) 0.5 Cmax (ng/mL) 1057 AUC0-t (ng/mL·h) 2185 AUC0-∞ (ng/mL·h) 2274 t1/2 (h) 1.6 MRT (h) 2.2 Animal Model: Sprague-Dawley rats[1] 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)[1] Dosage: 10mg/kg Administration: PO; daily for 19 days Result: Inhibited tumor growth with TGI of 132%. Animal Model: Male Balb/c mice[1] Dosage: 5 mg/kg Administration: IG, single dosage (Pharmacokinetic Analysis) Result: Exhibited favorable pharmacokinetic property.
References	[1]. Xiaolan ZHAN, et al. Three fused ring derivative-containing salt or crystal form and pharmaceutical composition thereof. WO2021104146A1 (example 22)

Molecular Formula	C₁₈H₁₉F₂N₅O₃S
Molecular Weight	423.44

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