Vulolisib 是一种有效且具有口服活性的磷脂酰肌醇 3 激酶 (PI3K)抑制剂，对 PI3Kα、PI3Kβ、PI3Kγ 和 PI3Kδ 的IC50分别为 0.2 nM、168 nM、90 nM 和 49 nM。对癌细胞具有抗增殖活性，也具有抗肿瘤活性。
| 生物活性 | Vulolisib is a potent and orally activephosphatidylinositol 3-kinase (PI3K)inhibitor, withIC50values of 0.2 nM, 168 nM, 90 nM and 49 nM forPI3Kα,PI3Kβ,PI3KγandPI3Kδ, respectively. Antiproliferative and antineoplastic activity[1]. |
| IC50& Target[1] | PI3Kα 0.2 nM (IC50) | PI3Kβ 168 nM (IC50) | PI3Kγ 90 nM (IC50) | PI3Kδ 49 nM (IC50) |
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体外研究
(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].
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体内研究
(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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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