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Cat. No.: HY-148521

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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.
(Pink: FLT3 and CDK9 Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker).

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

CAS No.: 3033084-05-5
Formula: C₄₇H₆₁N₁₃O₇
Molecular Weight:920.07

Storage:

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

Data Sheet (268 KB)

PROTAC FLT3/CDK9 degrader-1 Chemical Structure

CAS No.: 3033084-05-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

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]. (Pink: FLT3 and CDK9 Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker).

All PROTACs Isoforms :

All CDK Isoforms :

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.

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.

Chemical Information

CAS No. 3033084-05-5
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Řezníčková E, et al. Modulation of FLT3-ITD and CDK9 in acute myeloid leukaemia cells by novel proteolysis targeting chimera (PROTAC). Eur J Med Chem. 2022 Dec 5;243:114792. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC FLT3/CDK9 degrader-1

All PROTACs Isoforms

All CDK Isoforms