货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V58176-1ml	10mM in DMSO	￥3110.00 V58176-1ml ￥3110.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V58176-1ml

10mM in DMSO

￥3110.00

货期：3-5天

产品描述：

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.

靶点：

ALK5:<10 nM (IC50)

体外研究：

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[1].
ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels)[1].
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[1].
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[1].
ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model[1].

体内研究：

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.

保存条件：

-80°C 6个月;-20°C 1个月

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.418 ml	12.092 ml	24.185 ml
5 mM	0.484 ml	2.418 ml	4.837 ml
10 mM	0.242 ml	1.209 ml	2.418 ml
50 mM	0.048 ml	0.242 ml	0.484 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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