PeptideDB

FLT3-IN-28

FLT3-IN-28

CAS No.:

FLT3-IN-28 (Compound 12y) is an orally available FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits
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FLT3-IN-28 (Compound 12y) is an orally available FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells with FLT3 internal tandem duplication (ITD) mutations, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively (MV4-11 and MOLM-13/14 cell lines are acute myeloid leukemia (AML) cells carrying FLT3-ITD mutations). In addition, FLT3-IN-28 down-regulates the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induces cell cycle arrest and apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can dose-dependently prolong the survival rate in the MOLM-13 xenograft NSG mouse model. FLT3-IN-28 is expected to be used in the research of FLT3-ITD-related cancers.

Physicochemical Properties


Molecular Formula C23H19FN8O4
Molecular Weight 490.45
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets STAT5
References

[1]. Discovery of pyridine-based derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia. Eur J Med Chem. 2025 Feb 5;283:117173.


Solubility Data


Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0389 mL 10.1947 mL 20.3894 mL
5 mM 0.4078 mL 2.0389 mL 4.0779 mL
10 mM 0.2039 mL 1.0195 mL 2.0389 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.