HM43239 是一种具有口服活性和选择性FLT3抑制剂，IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性，并调节 p-STAT5, p-ERK Syk, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖并诱导其Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].

HM43239 potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation like MV4-11 (IC 50 : 1.3 nM), MOLM-13 (IC 50 : 5.1 nM), and MOLM-14 (IC 50 : 2.9 nM). Besides, HM43239 inhibits KG1a cells (CD34+/CD38- cells) proliferation [1]. HM43239 induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells) [1]. HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells [3].

HM43239 exhibits the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity [1]. HM43239 prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models [3].

2294874-49-8

C29H33ClN6

501.07

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years