2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. ALK5-IN-79

ALK5-IN-79 (compound 57) 是一种具有抗癌活性的 ALK 抑制剂，通过阻断 TGF-β1/SMAD 信号通路。ALK5-IN-79 减弱细胞外基质 (ECM) 的产生和胶原蛋白的沉积。ALK5-IN-79 具有良好的药代动力学特性和体内耐受性。

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ALK5-IN-79 Chemical Structure

ALK5-IN-79 Chemical Structure

CAS No. : 2725056-38-0

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ALK5-IN-79 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.

体外研究
(In Vitro)

ALK5-IN-79 (1000 nM；2 小时) 对 ALK5，SRC，LCK，BRAF (V600E)，ET，PDGFRα，EGFR 和 KDR 具有强至中度的抑制活性 (抑制率大于20%)[1]。
ALK5-IN-79 (0，0.125，0.25，0.5，1.0 and 2.0 μM；1 小时) 抑制 smad3 的磷酸化且呈剂量依赖性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ALK5-IN-79 相关抗体:

Western Blot Analysis[1]

Cell Line: Abnormal proliferation of cancer associated fibroblasts
Concentration: 0-2.0 μM
Incubation Time: 1 h
Result: ALK5-IN-79 blocked the TGF-β1 induced upregulation of collagen I (Col1) and α-SMA at mRNA and protein levels, i.e., the targeted genes of samd 3. ALK5-IN-79 led to the reduced secretion of Col 1.
体内研究
(In Vivo)

ALK5-IN-79 (300 mg/kg，每天腹腔注射连续 7 天) 没有使小鼠体重明显下降，具有体内深入研究安全性[1]。
ALK5-IN-79 (10 mg/kg 和 50 mg/kg 每隔一天静脉注射连续 24 天) 使用后肿瘤生长抑制率分别为 61.9% 和 80.5% 在 Syngeneic 模型中，ALK5-IN-79 (10 mg/kg 和 50 mg/kg 每隔一天筋脉注射连续 24 天) 使用后肿瘤生长抑制率分别为 62.1% 和 75.6% 在 PANC-1 皮下异种移植模型中。ALK5-IN-79 以剂量依赖的方式抑制胰腺癌肿瘤的生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pan02 syngeneic model and PANC-1 subcutaneous xenograft mode
Dosage: 10mg/kg and 50mg/kg ; every other day for 24 days
Administration: Intravenous injection (i.v.)
Result: Inhibited the growth of pancreatic cancer tumors in a dose-dependent manner
分子量

417.51

Formula

C23H27N7O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ALK5-IN-79 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ALK5-IN-792725056-38-0Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Pancreatic cancerActivin receptor-like kinase 5 inhibitor TGFβ1/SMAD signaling pathwayPan02 syngeneic model and PANC-1 subcutaneous xenograft modeALK5 InhibitorInhibitorinhibitorinhibit

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