CHR-6494 TFA [1458630-17-5]

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Cat# T9521-2mg

Size : 2mg

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Phone : +1 850 650 7790

Brand : TargetMol

Contact local distributor :

Phone : +1 850 650 7790

CHR-6494 TFA

Catalog No. T9521 CAS 1458630-17-5

CHR-6494 TFA is a potent haspin inhibitor, with an IC50 of 2 nM. It 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

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CHR-6494 TFA, CAS 1458630-17-5

Description	CHR-6494 TFA is a potent haspin inhibitor, with an IC50 of 2 nM. It 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
Targets&IC50	Haspin:2 nM (IC50)
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].

Molecular Weight	406.36
Formula	C18H17F3N6O2
CAS No.	1458630-17-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (135.35 mM)

References and Literature

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.

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CHR-6494 TFA 1458630-17-5 Others CHR-6494 inhibit apoptosis Haspin Kinase NRAS mutant melanoma cells CHR 6494 mitotic catastrophe Inhibitor mice CHR6494 cancer cells CHR6494 TFA BRAFV600E mutant melanoma cells CHR 6494 TFA inhibitor