Tuspetinib
Product Specifications
UNSPSC Description
Tuspetinib (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. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells[1][2][3].
Target Antigen
Apoptosis; FLT3
Type
Reference compound
Related Pathways
Apoptosis;Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/tuspetinib.html
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
ClC1=CN=C(NC2=CC(C3CC3)=CC(CN4C[C@H](N[C@H](C4)C)C)=C2)N=C1C5=CNC6=CC(C)=CC=C56
Molecular Weight
501.07
References & Citations
[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.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-145015/Tuspetinib-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-145015/Tuspetinib-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
2294874-49-8
Available Sizes
Curated Selection
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