CHR-6494 (TFA)
CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer[1][2][3].
Product Specifications
CAS Number
1458630-17-5
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
Target
Haspin Kinase
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/chr-6494-tfa.html
Solubility
10 mM in DMSO
Smiles
CCCNC1=NN2C(C3=CC4=C(C=C3)NN=C4)=CN=C2C=C1.OC(C(F)(F)F)=O
Molecular Formula
C18H17F3N6O2
Molecular Weight
406.36
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501
References & Citations
[1]Huertas D, et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene. 2012 Mar 15;31 (11) :1408-18.|[2]Han L, et al. Anti-Melanoma Activities of Haspin Inhibitor CHR-6494 Deployed as a Single Agent or in a Synergistic Combination with MEK Inhibitor. J Cancer. 2017 Aug 25;8 (15) :2933-2943.|[3]Chen A, et al. CRISPR/Cas9 screening identifies a kinetochore-microtubule dependent mechanism for Aurora-A inhibitor resistance in breast cancer. Cancer Commun (Lond) . 2021 Feb;41 (2) :121-139.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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