产品
编 号：F756000
分子式：C23H23N7O
分子量：413.48
分子式：C23H23N7O
分子量：413.48
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
10mg
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询价
结构图
CAS No: 2785430-90-0
产品详情
生物活性：
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
体内研究：
ALK5-IN-34 (EX-11) (oral; 10-100 mg/kg) reduces the phopho SMAD2 levels (p-SMAD2) in a dose dependent manner in A549 murine xenograft model.ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels).ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model and can delay progression.ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) and increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model and in Subcutaneous Cloudman S91 melanoma model.ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model.Animal Model:A549 murine xenograft model
Dosage:10, 50, 75 and 100 mg/kg
Administration:oral gavage
Result:Exhibited 92.5% inhibition based upon the average p-SMAD2 levels (75 mg/kg).
Animal Model:EMT6 Syngeneic TNBC Model
Dosage:75, 150 mg/kg
Administration:p.o., twice a day, for 21days
Result:Resulted significantly tumor growth inhibition (TGI) by 37% at 150 mg/kg.Result in significant tumor growth inhibition (TGI) with combination of anti-PD-LI and resulted in a significant increase in mean survival by 37%.Resulted in significant TGI by 34% with combination of anti-PD-1 and resulted in significant increase in mean survival by 26%.Decreased the intra-tumoral pressure.
Animal Model:Cachexia Model
Dosage:150 mg/kg
Administration:oral gavage, twice a day for 22 days
Result:Showed reduction in total fluid volume and high whole limb weights.
体外研究：
ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC50 value of ≤10 nM.ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC50 value of ＜100 nM.ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC50 value of ≤100 nM.ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent.ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner.ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2CI34W-driven growth in KGN and COV434 cells with IC50 values of 140 nM and >10 μM, respectively.ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line.ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent.ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent.
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.
体内研究：
ALK5-IN-34 (EX-11) (oral; 10-100 mg/kg) reduces the phopho SMAD2 levels (p-SMAD2) in a dose dependent manner in A549 murine xenograft model.ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels).ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model and can delay progression.ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) and increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model and in Subcutaneous Cloudman S91 melanoma model.ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model.Animal Model:A549 murine xenograft model
Dosage:10, 50, 75 and 100 mg/kg
Administration:oral gavage
Result:Exhibited 92.5% inhibition based upon the average p-SMAD2 levels (75 mg/kg).
Animal Model:EMT6 Syngeneic TNBC Model
Dosage:75, 150 mg/kg
Administration:p.o., twice a day, for 21days
Result:Resulted significantly tumor growth inhibition (TGI) by 37% at 150 mg/kg.Result in significant tumor growth inhibition (TGI) with combination of anti-PD-LI and resulted in a significant increase in mean survival by 37%.Resulted in significant TGI by 34% with combination of anti-PD-1 and resulted in significant increase in mean survival by 26%.Decreased the intra-tumoral pressure.
Animal Model:Cachexia Model
Dosage:150 mg/kg
Administration:oral gavage, twice a day for 22 days
Result:Showed reduction in total fluid volume and high whole limb weights.
体外研究：
ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC50 value of ≤10 nM.ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC50 value of ＜100 nM.ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC50 value of ≤100 nM.ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent.ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner.ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2CI34W-driven growth in KGN and COV434 cells with IC50 values of 140 nM and >10 μM, respectively.ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line.ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent.ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent.
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