HM43239 (Synonyms: HM43239) |
| Catalog No.GC63507 |
HM43239는 FLT3 WT, FLT3 내부 직렬 복제(ITD) 및 FLT3 D835Y 키나제에 대해 IC50이 각각 1.1nM, 1.8nM 및 1.0nM인 경구 활성 및 선택적 FLT3 억제제입니다. HM43239는 가역성 I형 억제제로서 FLT3의 키나제 활성을 억제하고 p-STAT5, p-ERK, SYK, JAK1/2 및 TAK1을 조절합니다. HM43239는 백혈병 세포의 증식을 억제하고 세포 사멸을 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2294874-49-8;2569527-64-4
Sample solution is provided at 25 µL, 10mM.
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HM43239 is an orally active and selective FLT3 inhibitor with IC50s 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 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, 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, such as MV4-11 (IC50: 1.3 nM), MOLM-13 (IC50: 5.1 nM), and MOLM-14 (IC50: 2.9 nM). HM43239 also 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 shows 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].
[1]. Miyoung Lee, et.al. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res July 1 2018 (78) (13 Supplement) 804.
[2]. Naval G. Daver, et.al. HM43239, a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations: Phase 1 /2 Study. Blood 2019; 134 (Supplement_1): 1331.
[3]. JiSook Kim, et.al. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res July 1 2019 (79) (13 Supplement) 1293.
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