1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FLT3 Apoptosis
  3. HI042

HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML).

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HI042

HI042 Chemical Structure

CAS No. : 898168-15-5

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Description

HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication (FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

FLT3

 

In Vitro

HI042 shows IC50 values for MOLM-13 cells were 0.88, 0.52, and 0.36 μM and >40, 1.03, and 0.64 μM for MV4-11 cells for the periods of 24, 48, and 72 h, respectively[1].
HI042 (0.3-5 μM, 7-10 days) reduces autonomous clonal growth in MOLM-13 and MV4-11 cells[1].
HI042 (0.25-4 μM, 72 h) induces cell apoptosis and disrupts in MOLM-13 and MV4-11 cells[1].
HI042 (0.25-1 μM, 72 h) induces cell differentiation in MOLM-13 and MV4-11 cells[1].
HI042 (0.06-1 μM, 72 h) significantly reduces the viability companied with Quizartinib (HY-13001) (0.12-2 nM) in MOLM-13 and MV4-11 cells[1].

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

Cell Viability Assay[1]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0.312, 0.625, 1.25, 2.5, 5, 10, 20, and 40 μM
Incubation Time: 24, 48 and 72 h
Result: Reduced cell viability in a time- and concentration dependent manner.

Apoptosis Analysis[1]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0.25, 0.5 1, 2 and 4 μM
Incubation Time: 72 h
Result: Increased the SubG1 cell population.
Increased PARP1 cleavage and γH2AX expression.

Cell Differentiation Assay[1]

Cell Line: MOLM-13 and MV4-11 cells
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 72 h
Result: Increased CD11b-positive cells.
Increased expression of the genes CEBPA and CEBPB.
Molecular Weight

301.32

Formula

C14H11N3O3S

CAS No.
SMILES

O=C(N/N=C/C1=CC=C([N+]([O-])=O)S1)/C=C/C2=CC=CC=C2

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
References
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HI042
Cat. No.:
HY-175473
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