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Tuspetinib (hydrate)

CAT: 0804-HY-145015ASize: 1 EachDry Ice: NoHazardous: No
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Description
Tuspetinib (HM43239) hydrate 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 hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells[1][2][3].
CAS Number
2758339-04-5
Product Name Alternative
HM43239 (hydrate)
UNSPSC
12352005
Target
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-hydrate.html
Solubility
10 mM in DMSO
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.O
Molecular Formula
C29H35ClN6O
Molecular Weight
519.08
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
Scientific Category
Reference compound1
Clinical Information
Phase 2

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T87582-01Tuspetinib hydrate
T212318-01Tuspetinib dihydrochloride
A20826-25Tuspetinib (HM-43239) 25mg
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A20826-100Tuspetinib (HM-43239) 100mg
A20826-10Tuspetinib (HM-43239) 10mg
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