1. Protein Tyrosine Kinase/RTK Apoptosis
  2. RET Apoptosis
  3. RET-IN-20

RET-IN-20 是一种有效的 RET 抑制剂,IC50 值为 13.7 nM。RET-IN-20 降低 p-Ret、p-Shc 蛋白的表达。RET-IN-20 诱导细胞凋亡 (apoptosis)。RET-IN-20 具有抗增殖和抗肿瘤活性。

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RET-IN-20 Chemical Structure

RET-IN-20 Chemical Structure

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RET-IN-20 is a potent RET inhibitor with an IC50 value of 13.7 nM. RET-IN-20 decreases the expression of p-Ret, p-Shc protein. RET-IN-20 induces apoptosis. RET-IN-20 shows antiproliferative and anti-tumor activity[1].

IC50 & Target

IC50: 3.7 nM (RET)[1]

体外研究
(In Vitro)

RET-IN-20 (compound 8q) (0, 1.2, 3.7, 11.1, 33.3, 100 nM; 4 h) 以剂量依赖性方式降低 p-Ret、p-Shc 蛋白的表达[1]
RET-IN-20 (0, 33.3, 100, 300 nM; 48 h) 以剂量依赖的方式诱导细胞凋亡[1]

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

Cell Proliferation Assay[1]

Cell Line: Ba/F3 RETWT, Ba/F3 RETV804M, Ba/F3 RETG810C, Ba/F3 RETG810R, Ba/F3 parental cells
Concentration: 0-10000 nM
Incubation Time: 72 h
Result: Showed antiproliferative activities with IC50s of 5.6, 24.4, 15.4, 53.2, >10000 nM for Ba/F3 RETWT, Ba/F3 RETV804M, Ba/F3 RETG810C, Ba/F3 RETG810R, Ba/F3 parental, respectively.

Apoptosis Analysis[1]

Cell Line: CCDC6-RET-WT, CCDC6-RET-V804M, CCDC6-RET-G810C, CCDC6-RET-G810R cells
Concentration: 0, 1.2, 3.7, 11.1, 33.3, 100 nM
Incubation Time: 4 h
Result: Inhibited the expression of p-Ret, p-Shc protein in a dose dependent manner.

Western Blot Analysis[1]

Cell Line: Ba/F3-CCDC6-RETG810 C/R cells
Concentration: 0, 33.3, 100, 300 nM
Incubation Time: 48 h
Result: Induced approximately 53.40% and 32.67% of cells undergoing apoptosis at a concentration of 300 nM in Ba/F3-CCDC6-RETG810C and Ba/F3-CCDC6-RETG810R cells, respectively.
体内研究
(In Vivo)

RET-IN-20 (10, 30 mg/kg; i.p.; once a day for 13 continuous days) 在小鼠体内显示出抗肿瘤活性[1]

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

Animal Model: CB17-SCID mice (Ba/F3-CCDC6-RETG810C tumor)[1]
Dosage: 10, 30 mg/kg
Administration: I.p.; once a day for 13 continuous days
Result: Suppressed tumor growth in a dose-dependent manner with tumor growth inhibition values (TGI) of 17.1% and 66.9%, respectively.
分子量

584.64

Formula

C32H33FN6O4

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

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产品名称:
RET-IN-20
目录号:
HY-151987
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