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.