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编 号：F750877
分子式：C24H31N5O4
分子量：453.53
分子式：C24H31N5O4
分子量：453.53
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CAS No: 2283349-24-4
产品详情
生物活性：
BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research.
体内研究：
BGB-8035 (7.5, 15, 30 mg/kg; 灌胃给药; 每天两次; 16 天) 表现出剂量依赖性抗肿瘤活性。 BGB-8035 (1, 3, 10, 30 mg/kg; 灌胃给药; 每天两次; 13 天) 在 8-9 周大的 Lewis 大鼠CIA 模型中以剂量依赖的方式抑制关节炎，并防止 CIA 模型相关的体重减轻。 Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs.Rats (IV; 1 mg/kg)Rats (PO; 5 mg/kg)Dogs (IV; 1 mg/kg)Dogs (PO; 2.5 mg/kg)
T1/2 (h)1.02.5
CL (mL/min/kg)24.46.89
Vss (L/kg)0.90.74
Tmax (h)0.250.42
Cmax (ng/mL)6671246
AUCinf (h?ng/mL)9642645
F (%)26.443
Animal Model:Female NOD/SCID mice at 9 weeks of age with REC-1 MCL xenografts
Dosage:7.5, 15, 30 mg/kg
Administration:PO; BID; 16 days
Result:Demonstrated dose-dependent antitumor activity, with TGI values of 64.1, 73.6, and 79.9%, respectively.
体外研究：
BGB-8035 对 HEK293 和 Ramos 细胞基本无毒 (IC50>10 μM)。
BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research.
体内研究：
BGB-8035 (7.5, 15, 30 mg/kg; 灌胃给药; 每天两次; 16 天) 表现出剂量依赖性抗肿瘤活性。 BGB-8035 (1, 3, 10, 30 mg/kg; 灌胃给药; 每天两次; 13 天) 在 8-9 周大的 Lewis 大鼠CIA 模型中以剂量依赖的方式抑制关节炎，并防止 CIA 模型相关的体重减轻。 Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs.Rats (IV; 1 mg/kg)Rats (PO; 5 mg/kg)Dogs (IV; 1 mg/kg)Dogs (PO; 2.5 mg/kg)
T1/2 (h)1.02.5
CL (mL/min/kg)24.46.89
Vss (L/kg)0.90.74
Tmax (h)0.250.42
Cmax (ng/mL)6671246
AUCinf (h?ng/mL)9642645
F (%)26.443
Animal Model:Female NOD/SCID mice at 9 weeks of age with REC-1 MCL xenografts
Dosage:7.5, 15, 30 mg/kg
Administration:PO; BID; 16 days
Result:Demonstrated dose-dependent antitumor activity, with TGI values of 64.1, 73.6, and 79.9%, respectively.
体外研究：
BGB-8035 对 HEK293 和 Ramos 细胞基本无毒 (IC50>10 μM)。
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