CHR 6494 trifluoroacetate  >98%

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产品简介:一种有效的选择性 haspin 抑制剂,IC50 值为 2 nM。CHR-6494 TFA 能够抑制组蛋白 H3T3 的磷酸化。CHR-6494 TFA 诱导黑色素瘤、乳腺癌等肿瘤细胞凋亡 (apoptosis)。CHR-6494 TFA 可用于癌症的研究。
溶解性:DMSO :55 mg/mL (135.35 mM) ( < 1 mg/mL refers to the product slightly soluble or insoluble )
靶点:haspin:2 nM (IC50)
体外研究: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.
体内研究:CHR-6494 (TFA; 50 mg/kg; i.p. in two cycles of five consecutive days for 15 days) inhibits the growth of tumor in 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.
保存条件:-20°C
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