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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 132 In Stock
5MG 195 In Stock
10MG 317 In Stock
25MG 530 In Stock
50MG 755 In Stock
100MG 1044 In Stock
500MG 2097 In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    CHR-6494 TFA
  • Note
    Research use only, not for human use.
  • Brief 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.
  • 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.(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.
  • In Vitro
    CHR-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.
  • In Vivo
    CHR-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.
  • Synonyms
    CHR 6494 TFA
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    DHODH
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1458630-17-5
  • Formula Weight
    406.362
  • Molecular Formula
    C18H17F3N6O2
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    OC(=O)C(F)(F)F.CCCNc1ccc2ncc(-c3ccc4[nH]ncc4c3)n2n1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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.
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