1. Protein Tyrosine Kinase/RTK Apoptosis
  2. Btk Apoptosis
  3. BTK-IN-7

BTK-IN-7 是一种有效的选择性 BTK 抑制剂 (IC50=4.0 nM),BTK-IN-7在酶 (ITK >250-fold, EGFR >2500-fold) 和细胞水平 (ITK >227-fold, EGFR 27-fold) 都具有较高的选择性。BTK-IN-7 还具有较高的抗肿瘤活性。

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BTK-IN-7 Chemical Structure

BTK-IN-7 Chemical Structure

CAS No. : 2952702-39-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity[1].

体外研究
(In Vitro)

BTK-IN-7 (compound 24a; 10, 100, 1000, 10000 nM; 48 hours) displays the antiproliferative effects in U-937 cells (IC50=3.6 μM)[1]. BTK-IN-7 (10, 100, 1000, 10000 nM; 48 hours; U937 cells) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1]. BTK-IN-7 (1-5 μM; 48 hours) induces apoptosis in U-937 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: U937, Ramos, Pfeiffer, Jeko-1 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 48 hours
Result: Displayed antiproliferative effects in U-937 (IC50=3.6 μM) cells.

Cell Cycle Analysis[1]

Cell Line: U937 cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: 48 hours
Result: Cells were arrested atthe G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: U937 cells
Concentration: 1, 2.5, 5 μM
Incubation Time: 48 hours
Result: An apoptosis rate was increased to 22.75% at a concentration of 5 μM.
体内研究
(In Vivo)

BTK-IN-7 (25 and 50 mg/kg; intraperitoneal injection; daily for 14 days) inhibits tumor growth in a dose-dependent manner in U-937 xenograft mouse model, and 50 mg/kg dosage displays a better antitumor effect[1].
BTK-IN-7 does not shows significant parenchymal injury or inflammatory cell infiltration in organs[1].

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

Animal Model: Male BALB/c nude mice (U397 xenograft mouse model) [1]
Dosage: 25, 50 mg/kg
Administration: Intraperitoneal injection; daily for 14 days
Result: Inhibited tumor growth in a dose-dependent manner and did not reveal significant parenchymal injury or inflammatory cell infiltration in organs.
分子量

540.61

Formula

C30H32N6O4

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
  • 摩尔计算器

  • 稀释计算器

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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:
BTK-IN-7
目录号:
HY-143900
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