
CHR-6494 TFA
CAS No. 1458630-17-5
CHR-6494 TFA( CHR 6494 TFA )
Catalog No. M28736 CAS No. 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.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 132 | In Stock |
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5MG | 195 | In Stock |
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10MG | 317 | In Stock |
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25MG | 530 | In Stock |
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50MG | 755 | In Stock |
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100MG | 1044 | In Stock |
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500MG | 2097 | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameCHR-6494 TFA
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NoteResearch use only, not for human use.
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Brief DescriptionCHR-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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DescriptionCHR-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.(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.(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.
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In VitroCHR-6494 (TFA; 0-105 nM; 72 hours) dose-dependently inhibits the growth of cancer cells, such as HCT-116, HeLa, MDA-MB-231, and Wi-38 cells, with IC50s of 500?nM, 473?nM, 752?nM and 1059 nM, respectively.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.CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36?h) is an inhibitor of angiogenesis in the ex vivo chicken embryo aortic arch ring assay.CHR-6494 (TFA) exhibits inhibitory activities against melanoma cell lines, including BRAFV600E mutants, NRAS mutants, and wild type cells, with IC50s ranging from 396 nM to 1229 nM.CHR-6494 (TFA; 300 nM and 600 nM; 72 hours) induces apoptosis, increases caspase 3/7 activity by 3- and 6-fold, respectively in COLO-792 cells, and to 8.5- and 16-fold in RPMI-7951 melanoma cells.CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells.CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237.
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In VivoCHR-6494 (TFA; 50?mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumorin nude mice bearing HCT-116 human colorectal cancer cells.CHR-6494 (TFA; 20 mg/kg; intraperitoneal injection for 15 consecutive days) inhibits the tumor growth in nude mice bearing MDA-MB-231 xenograft tumors. Animal Model:Male 4-5 weeks old athymic nu/nu mice harboring HCT-116 cells xenograft tumor with a tumor volume of 200?mm3 Dosage:50?mg/kg (diluted in a solution of 10% DMSO/20% 2-hydroxypropyl-b-cyclodextrin) Administration:i.p. in two cycles of five consecutive days for 15 days Result:Dose-dependent tumor growth inhibition was demonstrated. Animal Model:4‐week‐old female nude mice bearing MDA-MB-231 xenograft tumors Dosage:20 mg/kg in a final formulation in 10% DMSO/20% 2‐hydroxypropyl‐β‐cyclodextrin Administration:i.p. for 15 consecutive days Result:Inhibited the tumor volume and weight compared with the control group in nude mice bearing MDA-MB-231 xenograft tumors.Enhanced the tumor volume and weight inhibition of MLN8237 (20 mg/kg; p.o.) in vivo.
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SynonymsCHR 6494 TFA
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PathwayOthers
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TargetOther Targets
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RecptorDHODH
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Research Area——
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Indication——
Chemical Information
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CAS Number1458630-17-5
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Formula Weight406.362
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Molecular FormulaC18H17F3N6O2
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Purity>98% (HPLC)
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Solubility——
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SMILESOC(=O)C(F)(F)F.CCCNc1ccc2ncc(-c3ccc4[nH]ncc4c3)n2n1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Lolli ML, et al. New inhibitors of dihydroorotate dehydrogenase (DHODH) based on the 4-hydroxy-1,2,5-oxadiazol-3-yl (hydroxyfurazanyl) scaffold. Eur J Med Chem. 2012 Mar;49:102-9.
molnova catalog



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