Home>>Signaling Pathways>> TGF-β / Smad Signaling>>ALK5-IN-34

ALK5-IN-34

目录号 : GC73338

ALK5-IN-34是一种选择性口服活性激活素受体样激酶(ALK)抑制剂。

ALK5-IN-34 Chemical Structure

Cas No.:2785430-90-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,948.00
现货
1 mg
¥1,260.00
现货
5 mg
¥3,240.00
现货
10 mg
¥5,130.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

Description

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.

ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC50 value of ≤10 nM[1].ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC50 value of <100 nM[1].ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC50 value of ≤100 nM[1].ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent[1].ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner[1].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[1].ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line[1].ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent[1].ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent[1].

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].

References:
[1]. Bettina FRANZ, et al. Alk-5 inhibitors and uses thereof. Patent. WO2022126133A1.

化学性质

Cas No. 2785430-90-0 SDF
分子式 C23H23N7O 分子量 413.48
溶解度 DMSO : 100 mg/mL (241.85 mM; Need ultrasonic) 储存条件 -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.4185 mL 12.0925 mL 24.185 mL
5 mM 0.4837 mL 2.4185 mL 4.837 mL
10 mM 0.2418 mL 1.2092 mL 2.4185 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

产品文档

Quality Control & SDS

View current batch: