(1E)-CFI-400437 dihydrochloride 是一种有效的PLK4(IC50= 0.6 nM)，并对 PLK 家族的其他成员有选择性 (>10 μM)。(1E)-CFI-400437 dihydrochloride 抑制 Aurora A、 Aurora B、 KDR 和 FLT-3，IC50分别为 0.37、0.21、0.48 和 0.18 μM。具有抗增殖活性。
| 生物活性 | (1E)-CFI-400437 dihydrochloride is a potentPLK4(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 andFLT-3with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity[1]. |
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体内研究
(In Vivo) | (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 ngoh/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%[1].
| Animal Model: | 6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model)[1] | | Dosage: | 25 mg/kg | | Administration: | Intraperitoneal injection; daily for 21 days | | Result: | Effective in a mouse xenograft model of tumor growth.
In this study, (1E)-CFI-400437 is weighed and suspended in PEG400:water (30:70) and sonicated at rt for 30 min. The compound is dispensed in aliquots and stored at –20 C° for the duration of the study, and each aliquot was thawed at room temperature before each dose. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(22.10 mM;Need ultrasonic) H2O : 1 mg/mL(1.77 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 1.7684 mL | 8.8419 mL | 17.6838 mL | | 5 mM | 0.3537 mL | 1.7684 mL | 3.5368 mL | | 10 mM | 0.1768 mL | 0.8842 mL | 1.7684 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
