CHR-6494 TFA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CHR-6494 TFA 是一种有效的 haspin 抑制剂，IC50 为 2 nM。它抑制组蛋白 H3T3 磷酸化。 CHR-6494 TFA 诱导癌细胞凋亡，包括黑色素瘤和乳腺癌。 CHR-6494 TFA可用于癌症研究。

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.

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.

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.

CHR 6494 TFA

Others

Other Targets

DHODH

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1458630-17-5

406.362

C18H17F3N6O2

>98% (HPLC)

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OC(=O)C(F)(F)F.CCCNc1ccc2ncc(-c3ccc4[nH]ncc4c3)n2n1

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(-20℃)

With Ice Pack

≥ 2 years