CHR-6494,1458630-17-5

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CHR-6494 TFA

CAS No. : 1458630-17-5

MCE 国际站：CHR-6494 TFA

产品活性：CHR-6494 TFA 是一种有效的选择性 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。

研究领域：Cell Cycle/DNA Damage

作用靶点：Haspin Kinase

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 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.

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