产品
编 号：F752011
分子式：C22H23BrN8OS
分子量：527.44
分子式：C22H23BrN8OS
分子量：527.44
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: 2396465-33-9
产品详情
生物活性：
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.
体内研究：
GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose.GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model.Animal Model:Balb/c mice injected with RENCA cells
Dosage:15 mg/kg
Administration:Oral gavage; 15 mg/kg; BID; 17 days
Result:Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues.Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.
Animal Model:LL2 syngeneic mouse model
Dosage:50 mg/kg
Administration:Oral gavage; 50 mg/kg; BID; 17 days
Result:Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.
体外研究：
GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation.
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.
体内研究：
GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose.GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model.Animal Model:Balb/c mice injected with RENCA cells
Dosage:15 mg/kg
Administration:Oral gavage; 15 mg/kg; BID; 17 days
Result:Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues.Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.
Animal Model:LL2 syngeneic mouse model
Dosage:50 mg/kg
Administration:Oral gavage; 50 mg/kg; BID; 17 days
Result:Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.
体外研究：
GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备