CHR-6494 (TFA)

• Description :

  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].

• 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