(1E)-CFI-400437 dihydrochloride |
| カタログ番号GC62728 |
(1E)-CFI-400437 二塩酸塩は、強力な PLK4 (IC50 = 0.6 nM) 阻害剤であり、PLK ファミリーの他のメンバーに対して選択的です (>10 μM)。 (1E)-CFI-400437 二塩酸塩は、Aurora A、Aurora B、KDR、および FLT-3 を、それぞれ 0.37、0.21、0.48、および 0.18 μM の IC50 で阻害します。抗増殖活性。
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Cas No.: 1247000-76-5
Sample solution is provided at 25 µL, 10mM.
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(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity[1].
(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth[1].The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng•h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%[1].
[1]. Laufer R, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56(15):6069-6087.
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