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。
| 生物活性 | CHR-6494 TFA is a potent inhibitor ofhaspin, with anIC50of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces theapoptosisofcancercells, including melanoma and breastcancer. CHR-6494 TFA can be used in the research ofcancer[1][2][3]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | CHR-6494 (TFA; 0-105nM; 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[1].
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[1].
CHR-6494 (TFA; 0, 0.5, 1.0 μM; 24 to 36 h) is an inhibitor of angiogenesis in theex vivochicken embryo aortic arch ring assay[1].
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[2].
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[2].
CHR-6494 (TFA; 50, 200 nM; 1 week) enhances the antiproliferative effects of MLN8237 in MDA-MB-231, SKBR3 breast cancer cells[3].
CHR-6494 (TFA; 200 nM; 72 hours) enhances the apoptosis of MDA-MB-231 and SKBR3 cells when combined with MLN8237[3].
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体内研究
(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[1].
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[3].
| Animal Model: | Male 4-5 weeks old athymicnu/numice harboring HCT-116 cells xenograft tumor with a tumor volume of 200 mm3[1] | | 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.
Did not change the body weight of mice. |
| 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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