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: 2025-08-31 20:06:58
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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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C18H19F2N5O3S |
|---|---|
| Molecular Weight | 423.44 |