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 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.

For research use only. We do not sell to patients.

PROTAC FLT3/CDK9 degrader-1 Chemical Structure

PROTAC FLT3/CDK9 degrader-1 Chemical Structure

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Description

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].

In Vitro

PROTAC FLT3/CDK9 degrader-1 (compound PROTAC 13) (0.004, 0.02, 0.1, 0.5, 2.5 µM; 16 h) decreases the expression of p-FLT3 Y589/591, p-STAT5 Y694, p-ERK1/2 T202/Y204 and induces apoptosis in a dose-dependent manner in MV4-11 cells[1].
PROTAC FLT3/CDK9 degrader-1 (0, 0.1, 0.5 µM; 16 h) decreases the degradation of target proteins when is pre-treated for 90 min with MG132 (HY-13259) (0.2 µM) in MV4-11 cells[1].

MedChemExpress (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.
Molecular Weight

920.07

Formula

C47H61N13O7

SMILES

NC(CC1)CCC1NC2=NC(NC(C=C3)=CC=C3N(CC4)CCN4CCOCCOCCNC(CNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)=C8C(N(C9CCCC9)C=N8)=N2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PROTAC FLT3/CDK9 degrader-1 Related Classifications

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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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Product Name:
PROTAC FLT3/CDK9 degrader-1
Cat. No.:
HY-148521
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