2. PROTAC Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage JAK/STAT Signaling Stem Cell/Wnt MAPK/ERK Pathway Apoptosis PI3K/Akt/mTOR
  3. PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt
  4. 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 MV-4-11 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/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)).

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

PROTAC FLT3/CHK1 Degrader-1

PROTAC FLT3/CHK1 Degrader-1 Chemical Structure

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PROTAC FLT3/CHK1 Degrader-1 Related Antibodies

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Description

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 MV-4-11 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/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238))[1].

IC50 & Target[1]

Chk1

4.17 nM (DC50)

FLT3

5.88 nM (DC50)

Cereblon

 

In Vitro

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.

PROTAC FLT3/CHK1 Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 5, 20, 50, 100 nM
Incubation Time: 0, 3, 6, 9, 12 h
Result: Downregulated FLT3 and CHK1.
Inhibited phosphorylation of downstream effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204).
Downregulated c-Myc, and maintains p53 expression.
In Vivo

PROTAC FLT3/CHK1 Degrader-1 (Compound A28) (5-10 mg/kg, i.v., once weekly for 21 days) demonstrates significant tumor growth suppression in mice bearing MV-4-11 subcutaneous xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NU/NU mice (18-25 g) bearing MV-4-11 subcutaneous xenografts[1]
Dosage: 5, 10 mg/kg
Administration: i.v., once weekly for 21 days
Result: Achieved tumor growth.
Showed no significant changes in body weight.
Molecular Weight

782.78

Formula

C38H42F4N8O6
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
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/CHK1 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/CHK1 Degrader-1PROTACsFLT3Checkpoint Kinase (Chk)STATERKc-MycAktCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Extracellular signal regulated kinasesMycPKBProtein kinase Bacute myeloid leukemiaFLT3/CHK1PROTACMV-4-11 cellsInhibitorinhibitorinhibit

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