1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK PROTAC Apoptosis
  2. CDK FLT3 PROTACs Apoptosis
  3. PROTAC FLT3/CDK9 degrader-1

PROTAC FLT3/CDK9 degrader-1 是一种有效的 FLT3CDK9PROTAC 降解剂。PROTAC FLT3/CDK9 degrader-1 诱导细胞凋亡 (Apoptosis) 并有效降解靶蛋白 FLT3 和 CDK9。PROTAC FLT3/CDK9 degrader-1具有研究 FLT3-ITD 突变型 AML 的潜力。

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PROTAC FLT3/CDK9 degrader-1 Chemical Structure

PROTAC FLT3/CDK9 degrader-1 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML[1].

体外研究
(In Vitro)

PROTAC FLT3/CDK9 degrader-1 (compound PROTAC 13) (0.004, 0.02, 0.1, 0.5, 2.5 µM; 16 h) 降低 p-FLT3 Y589/591、p-STAT5 Y694、p-ERK1/2 T202/Y204 的表达,并以剂量依赖性方式诱导 MV4-11 细胞凋亡[1]
在 MV4-11 细胞中用 MG132 (HY-13259) (0.2 µM) 预处理 90 分钟后,PROTAC FLT3/CDK9 degrader-1 (0, 0.1, 0.5 µM; 16 h) 的蛋白降解能力减弱[1]

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

Cell Proliferation Assay[1]

Cell Line: MV4-11, MV4-11 CRBN-def., MOLM-13, RS4-11, HL60, U937, THP-1, Kasumi-1, CEM, K562 cells
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.047, 0.119, 0.042, 1.014, 6.122, 9.507, 9.993, >10, >10, >10 µM for MV4-11, MV4-11 CRBN-def., MOLM-13, RS4-11, HL60, U937, THP-1, Kasumi-1, CEM, K562 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.004, 0.02, 0.1, 0.5, 2.5 µM
Incubation Time: 16 h
Result: Decreased the expression of p-FLT3 Y589/591, p-STAT5 Y694, p-ERK1/2 T202/Y204 in a dose-depent manner.

Apoptosis Analysis[1]

Cell Line: MV4-11, CRBN-deficient MV4-11 cells
Concentration: 0.004, 0.02, 0.1, 0.5, 2.5 µM
Incubation Time: 16 h
Result: Induced apoptosis with the activities of caspases 3 and 7 increased in a concentration-dependent manner in MV4-11 cells.
分子量

920.07

Formula

C47H61N13O7

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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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)
× = ×
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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:
PROTAC FLT3/CDK9 degrader-1
目录号:
HY-148521
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