YS-370 |
カタログ番号GC65184 |
YS-370 (化合物 44) は、P-糖タンパク質 (P-gp) の強力で選択性の高い経口活性阻害剤です。 YS-370 は P-gp ATPase 活性を刺激し、CYP3A4 に対して中程度の阻害を示します。 YS-370 は、SW620/AD300 および HEK293T-ABCB1 細胞のパクリタキセルおよびコルヒチンに対する多剤耐性 (MDR) を効果的に逆転させます。パクリタキセルと組み合わせたYS-370は、はるかに強力な抗腫瘍活性を達成します。
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Cas No.: 2470908-79-1
Sample solution is provided at 25 µL, 10mM.
YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity[1].
[1]. Yuan S, et al. Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors. J Med Chem. 2021;64(19):14895-14911.
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