Clifutinib
Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM) . Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia[1].
Product Specifications
CAS Number
[1862226-99-0]
UNSPSC
12352005
Target
Akt; Apoptosis; FLT3; JAK; p38 MAPK; PI3K; Ras; STAT
Related Pathways
Apoptosis; Epigenetics; GPCR/G Protein; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Purity
99.59
Solubility
DMSO : 25 mg/mL (ultrasonic)
Smiles
O=C(NC1=NOC(C(C)(C)C)=C1)NC2=CC=C(C#CC3=CC=C(OCCCN4CCOCC4)C=C3)C=C2
Molecular Formula
C29H34N4O4
Molecular Weight
502.60
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Available Sizes
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