| Name | HM43239 |
| Description | 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]. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (99.79 mM)
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| Keywords | HM 43239 | HM-43239 | HM43239 |
| Inhibitors Related | UNC2025 | Gilteritinib | Fedratinib | Nintedanib | Sunitinib | Sunitinib Malate | Sorafenib | Tandutinib | Pexidartinib | KW-2449 | Sorafenib tosylate | SGI-1776 |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
