产品
编 号：F751971
分子式：C18H19F2N5O3S
分子量：423.44
分子式：C18H19F2N5O3S
分子量：423.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2390105-79-8
产品详情
生物活性：
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.
体内研究：
Vulolisib (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)
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
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.
体外研究：
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.
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.
体内研究：
Vulolisib (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)
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
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.
体外研究：
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.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备