2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. FLT3 Checkpoint Kinase (Chk)
  4. FLT3/CHK1-IN-2

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML).

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

FLT3/CHK1-IN-2

FLT3/CHK1-IN-2 Chemical Structure

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FLT3/CHK1-IN-2 Related Antibodies

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Description

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML)[1].

Cellular Effect
Cell Line Type Value Description References
BaF3 IC50
26.37 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
28.96 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 F691L mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
29.3 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835F mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 D835F mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
30.24 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
BaF3 IC50
75.81 nM
Compound: 30
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against mouse BaF3 cells expressing FLT3 ITD D835Y mutant assessed as inhibition of cell growth incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
MV4-11 IC50
2.96 nM
Compound: 30
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader
Antiproliferative activity against human MV4-11 cells expressing FLT3 ITD/TKD mutant incubated for 72 hrs by absorbance based microplate reader
[PMID: 38389894]
In Vitro

FLT3/CHK1-IN-2 shows antiproliferation activity against MV4-11 cell (IC50: <4 nM)[1].
FLT3/CHK1-IN-2 shows antiproliferative activity against BaF3 cells with a variety of FLT3 mutations (IC50: 28.96, 29.30, 26.37, 30.24, 75.81 nM for BaF3-FLT3-F691L, BaF3-FLT3-D835F, BaF3-FLT3-D835V, BaF3-FLT3-ITD, BaF3-FLT3-ITD/D835Y cells)[1].
FLT3/CHK1-IN-2 (0-100 nM) inhibits the phosphorylation of FLT3 and its main downstream effectors, STAT5 (Tyr694), AKT (Ser473) and ERK (Tyr204) in MV4-11 cells, and decreases the pS296-CHK1 level and the c-Myc protein expression level[1].

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

FLT3/CHK1-IN-2 Related Antibodies
In Vivo

FLT3/CHK1-IN-2 (20 mg/kg, p.o.) has favorable PK properties, with the Cmax of 2213.07 ng/mL, and the AUC(0−t) of 2736.58 h·ng/mL[1].

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

444.47

Formula

C18H23F3N6O2S
SMILES

NCCCNC1=NC(NC2=CC(CCN(S(=O)(C)=O)C3)=C3C=C2)=NC=C1C(F)(F)F
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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FLT3/CHK1-IN-2 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:

FLT3/CHK1-IN-2FLT3Checkpoint Kinase (Chk)Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3MV4-11 AMLInhibitorinhibitorinhibit

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