Luvixasertib
CFI-402257 is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50 of 1.7 nM for TTK in vitro. CFI-402257 has anti-cancer activity[1].
Product Specifications
CAS Number
1610759-22-2
Product Name Alternative
CFI-402257
UNSPSC
12352005
Hazard Statement
H315, H319, H320
Target
Mps1
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; Cytoskeleton
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/CFI-402257.html
Purity
99.9600
Solubility
DMSO : 1.67 mg/mL (ultrasonic)
Smiles
CC1=CC(C2=C3N=C(OC4=CN=CC=C4)C=C(NC[C@@H]5C[C@@](O)(C)C5)N3N=C2)=CC=C1C(NC6CC6)=O
Molecular Formula
C28H30N6O3
Molecular Weight
498.58
Precautions
H315, H319, H320
References & Citations
[1]Liu Y, et al. Discovery of Pyrazolo[1,5-a]pyrimidine TTK Inhibitors: CFI-402257 is a Potent, Selective, Bioavailable Anticancer Agent. ACS Med Chem Lett. 2016 May 6;7 (7) :671-5.|[2]Mason JM, et al. Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer. Proc Natl Acad Sci U S A. 2017 Mar 21;114 (12) :3127-3132.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Citation 01
BioRxiv. 2021 Feb 5.|bioRxiv. 2020 Apr. |Cancer Discov. 2019 Feb;9 (2) :230-247.|Commun Biol. 2021 May 24;4 (1) :617.|Oncol Rep. 2024 Aug;52 (2) :101.|Front Oncol. 2024 Aug 9:14:1447807.
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