2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. FLT3-IN-18

FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML).

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FLT3-IN-18 Chemical Structure

FLT3-IN-18 Chemical Structure

CAS No. : 752191-77-8

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FLT3-IN-18 Related Antibodies

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Description

FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML)[1].

IC50 & Target

IC50: 0.003 µM (FLT3)[1]
In Vitro

FLT3-IN-18 (compound 7d) (0, 0.01, 0.1, 1, 10, 100 nM; 1h) decreases the protein expression of p-FLT3 Y589/591, p-FLT3 Y842, p-TAT5 Y694, p-ERK1/2 T202/Y204, and p-MEK1/2 S217/221, p-AKT S473 in a dose-dependent manner in MV4-11 cells[1].
FLT3-IN-18 (0, 0.01, 0.1, 1, 10, 100 nM; 24 h) induces apoptosis and cell cycle arrest at G1 phase[1].

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

FLT3-IN-18 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Inhibited cell growth with GI50s of 0.002, 0.380, 0.001, 0.513, 0.713, 0.664, 0.197 µM for MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time: 1 h
Result: Decreased the expression of p-FLT3 Y589/591, p-FLT3 Y842, p-TAT5 Y694, p-ERK1/2 T202/Y204, and p-MEK1/2 S217/221, p-AKT S473 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time: 24 h
Result: Induced cell cycle arrest at G1 phase.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0, 0.01, 0.1, 1, 10, 100 nM
Incubation Time: 24 h
Result: Increased cleavage of the apoptotic marker protein PARP-1 (89 kDa fragment) and educed levels of the antiapoptotic protein Mcl-1.
In Vivo

FLT3-IN-18 (10 mg/kg; i.p.; once) effectively inhibits FLT3 and STAT5 phosphorylation in rats[1].

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

Animal Model: Rats (MV4-11 xenografts)[1]
Dosage: 10 mg/kg
Administration: I.p.; once
Result: Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts, reduced STAT5 phosphorylation by over 95% after 24 h.
Molecular Weight

476.62

Formula

C26H36N8O
CAS No.
SMILES

N[C@H](CC1)CC[C@@H]1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3)=C5N=CN(C6CCCC6)C5=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
References
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FLT3-IN-18 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-IN-18752191-77-8FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3anti-proliferativeMV4-11apoptosisG1 phasep-STAT5AMLInhibitorinhibitorinhibit

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