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 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

PROTAC FLT3/CDK9 degrader-1 Chemical Structure

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PROTAC FLT3/CDK9 degrader-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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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].

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]
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.

PROTAC FLT3/CDK9 degrader-1 Related Antibodies

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
Shipping

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.

Keywords:

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

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