PROTAC FLT3/CHK1 Degrader-1
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces Apoptosis in cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML).
(Pink: FLT3 and Checkpoint Kinase (Chk) ligand (HY-178869); Blue: Cereblon ligand (HY-W093272); Black: linker).
For research use only. We do not sell to patients.
- Formula: C38H42F4N8O6
- Molecular Weight:782.78
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
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Chk1 4.17 nM (DC50) |
FLT3 5.88 nM (DC50) |
Cereblon |
STAT5 |
PROTAC FLT3/CHK1 Degrader-1 (Compound A28) (0-50 nM, 16 h) degrades FLT3 and CHK1 in a concentration-dependent manner in MV-4-11 cells, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively[1].
PROTAC FLT3/CHK1 Degrader-1 (5-100 nM, 0-12 h) downregulates FLT3 and inhibits phosphorylation of downstream effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204) in a concentration- and time-dependent manner in MV-4-11 cells[1].
PROTAC FLT3/CHK1 Degrader-1 (5-100 nM, 0-12 h) degrades CHK1, downregulates c-Myc, and maintains p53 expression in MV-4-11 cells[1].
PROTAC FLT3/CHK1 Degrader-1 exhibits potent antiproliferative activity against FLT3-mutated cells (MV-4-11, MOLM-13, BaF3-FLT3-F691L/D835V/D835F/ITD/ITD/D835Y) and weak activity against non-FLT3-mutated cancer cells (THP-1, TF-1, HL-60)[1].
PROTAC FLT3/CHK1 Degrader-1 (1-5 μM, 24 h) induces apoptosis in MV-4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells
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Concentration:5, 20, 50, 100 nM
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Incubation Time:0, 3, 6, 9, 12 h
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Result:Downregulated FLT3 and CHK1.
Inhibited phosphorylation of downstream effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204).
Downregulated c-Myc, and maintains p53 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NU/NU mice (18-25 g) bearing MV-4-11 subcutaneous xenografts[1]
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Dosage:5, 10 mg/kg
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Administration:i.v., once weekly for 21 days
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Result:Achieved tumor growth.
Showed no significant changes in body weight.
Chemical Information
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Molecular Weight 782.78
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Formula C38H42F4N8O6
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SMILES
O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=C(N4CC(CN[C@H]5CC[C@@H](NC6=NC(NC7=CC=C(OCC(C)(O)C)C=C7)=NC=C6C(F)(F)F)CC5)C4)C(F)=C3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC FLT3/CHK1 Degrader-1 Related Classifications
HY-178858 Related Classifications
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