TCS7010 is an exceptionally selective inhibitor of Aurora A kinases, distinguishing itself by not inhibiting Aurora B. This specificity makes TCS7010 a valuable tool compound for studying the specific cellular roles of Aurora A kinases without the confounding effects of Aurora B inhibition[1].
体外研究
TCS7010 is an exceptionally selective inhibitor of Aurora A kinases, distinguishing itself by not inhibiting Aurora B. This specificity makes TCS7010 a valuable tool compound for studying the specific cellular roles of Aurora A kinases without the confounding effects of Aurora B inhibition[1].
TCS7010 细胞实验
Cell Line
Concentration
Treated Time
Description
References
NCI-H82 cells
1.0 µM
24 hours
To evaluate the effect of the compound on cMYC and MYCN protein levels, results showed that compound 13 significantly reduced cMYC and MYCN levels at 1.0 μM concentration.
J Med Chem. 2021 Jun 10;64(11):7312-7330.
SK-N-BE(2) cells
1.0 µM
24 hours
To evaluate the effect of the compound on cMYC and MYCN protein levels, results showed that compound 13 significantly reduced cMYC and MYCN levels at 1.0 μM concentration.
J Med Chem. 2021 Jun 10;64(11):7312-7330.
A673 cells
2 µM
72 hours
To screen compounds with anticancer activity, TCS7010 exhibited significant anticancer activity.
Cell Death Dis. 2024 Jan 29;15(1):99.
TCS7010 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
A673 xenograft model
Intraperitoneal injection
40 mg/kg/d
Once daily for 14 days
TCS7010 significantly inhibited ES growth in vivo.
Cell Death Dis. 2024 Jan 29;15(1):99.
Athymic nude (nu/nu) mice
NCI-H446 xenograft model
Intravenous injection
50 mg/kg
5-on-2-off dosing schedule for two consecutive weeks
To evaluate the in vivo antitumor efficacy of compound 13, results showed that at a dose of 50 mg/kg, tumor growth inhibition exceeded 90%.
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