CHR-6494 TFA

SKU: orb1298045

Description

CHR-6494 TFA is a potent and selective haspin inhibitor (IC50 = 2 nM) that blocks histone H3T3 phosphorylation. It induces apoptosis in various cancer cell lines, such as melanoma and breast cancer, in vitro, supporting its use as a research tool for oncology studies.

Research Area

Cell Biology

Key Properties

• CAS Number: 1458630-17-5
• MW: 406.36
• Purity: 99.50% (May vary between batches)
• Formula: C₁₈H₁₇F₃N₆O₂
• SMILES: CCCNC1=NN2C(C=C1)=NC=C2C3=CC4=C(NN=C4)C=C3.O=C(O)C(F)(F)F
• Target: Others,Haspin Kinase
• Solubility: DMSO:55 mg/mL (135.35 mM)

Bioactivity

• Target IC50:
  Haspin:2 nM (IC50)
• In Vivo:
  Administration of CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor and no obvious body weight change is observed in nude mice bearing HCT-116 human colorectal cancer cells.
• In Vitro:
  Administration of CHR-6494 (TFA; 0-10-5 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with an IC50s of 500 nM, 473 nM, 752 nM and 1059 nM, respectively. Administration of CHR-6494 (TFA; 500 nM) produces a mitotic catastrophe with abnormal morphology of the mitotic spindle and centrosome amplification, and upregulates the spindle assembly checkpoint protein BUB1 and the marker of mitotic arrest cyclin B1.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

apoptosis, BRAFV600E mutant melanoma cells, cancer cells, CHR 6494, CHR 6494 TFA, CHR6494, CHR-6494, CHR6494 TFA, CHR-6494 TFA, mice, mitotic catastrophe, Inhibitor, NRAS mutant melanoma cells, inhibit, Haspin Kinase

Compound Identifiers

PubChem CID

91691123