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

PROTAC FLT3/CDK9 degrader-1 是一种有效的 FLT3 和 CDK9 双 PROTAC 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

PROTAC FLT3/CDK9 degrader-1 Chemical Structure

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PROTAC FLT3/CDK9 degrader-1 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 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].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM GI50
> 10 μM
Compound: 13
Antiproliferative activity against human CEM cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human CEM cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
HL-60 GI50
6.122 μM
Compound: 13
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
K562 GI50
> 10 μM
Compound: 13
Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
Kasumi 1 GI50
> 10 μM
Compound: 13
Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
MOLM-13 GI50
0.042 μM
Compound: 13
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutation assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutation assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
MV4-11 GI50
0.047 μM
Compound: 13
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutation assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutation assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
MV4-11 GI50
0.119 μM
Compound: 13
Antiproliferative activity against CRBN-deficient human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against CRBN-deficient human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
RS4-11 GI50
1.014 μM
Compound: 13
Antiproliferative activity against human RS4-11 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human RS4-11 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
THP-1 GI50
9.993 μM
Compound: 13
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
U-937 GI50
9.507 μM
Compound: 13
Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
Antiproliferative activity against human U-937 cells assessed as cell growth inhibition incubated for 72 hrs by resazurin dye based fluorescence analysis
[PMID: 36191408]
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.

PROTAC FLT3/CDK9 degrader-1 相关抗体:

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

PROTAC FLT3/CDK9 degrader-1 相关分类

  • 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.

Keywords:

PROTAC FLT3/CDK9 degrader-1CDKFLT3PROTACsApoptosisCyclin dependent kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3apoptosisCDK9MV4-11caspases 3/7AMLInhibitorinhibitorinhibit

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