FLT3

CHMFL-FLT3-122 is a selective FLT3 kinase inhibitor with an IC50 of 40 nM. It demonstrates significant selectivity for FLT3 over BTK and c-KIT, exhibiting IC50 values of 421 nM and 559 nM, respectively. This compound effectively induces apoptosis through cell cycle arrest in the G0/G1 phase, making it a valuable tool for research in hematological malignancies and targeted cancer therapies.

Tandutinib hydrochloride is a potent and selective inhibitor of FLT3, with an IC50 of 0.22 μM. This compound also exhibits inhibitory activity against c-Kit and PDGFR, with IC50 values of 0.17 μM and 0.20 μM, respectively. Its primary applications include research in acute myelogenous leukemia (AML). Additionally, Tandutinib hydrochloride demonstrates the ability to cross the blood-brain barrier, making it a valuable tool in studying central nervous system involvement in malignancies.

Flonoltinib TFA is a potent and orally bioavailable inhibitor that targets both JAK2 and FLT3, exhibiting IC50 values of 0.7 nM and 4 nM, respectively, alongside 26 nM and 39 nM for JAK1 and JAK3. This compound possesses significant anti-cancer activity, making it a valuable tool for research in oncology and therapeutic development against malignancies driven by these pathways. Its dual inhibition profile highlights its potential in addressing cancers associated with aberrant JAK2 and FLT3 signaling.

Ruserontinib is an orally active multikinase inhibitor targeting EGFR, FLT3, and Abl. With an IC50 of 55 nM for human FLT3, it demonstrates significant antitumor activity. This compound is primarily utilized in cancer research, particularly for studying the effects of inhibiting key kinases involved in tumor progression and survival.

FLT3-IN-40 is a type I ATP-competitive inhibitor of FLT3, demonstrating an IC50 of 16.26 nM. This compound effectively reduces FLT3 autophosphorylation and downregulates ERK phosphorylation, thereby exhibiting significant antiproliferative activity, influencing cell cycle regulation, and promoting apoptosis. FLT3-IN-40 is particularly valuable for research applications focused on acute myeloid leukemia.