| Name | CHR-6494 TFA |
| Description | CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research. |
| 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[1]. 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[1]. |
| 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[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 55 mg/mL (135.35 mM), Sonication is recommended.
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| Keywords | NRAS mutant melanoma cells | mitotic catastrophe | mice | Inhibitor | inhibit | Haspin Kinase | CHR-6494 TFA | CHR6494 TFA | CHR-6494 | CHR6494 | CHR 6494 TFA | CHR 6494 | cancer cells | BRAFV600E mutant melanoma cells | apoptosis |
| Inhibitors Related | LDN-209929 dihydrochloride | Haspin-IN-2 | INE963 | MU1920 | Haspin-IN-3 | AZ1495 | Haspin-IN-1 | Haspin-IN-4 | MELK-8a | CHR-6494 | LDN-192960 hydrochloride | LDN-192960 |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |