(1E)-CFI-400437 dihydrochloride

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(1E)-CFI-400437 dihydrochloride  纯度: 98.89%

(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。

(1E)-CFI-400437 dihydrochloride

(1E)-CFI-400437 dihydrochloride Chemical Structure

CAS No. : 1247000-76-5

规格 价格 是否有货 数量
5 mg ￥2100 In-stock
10 mg ￥3200 In-stock
25 mg ￥6500 In-stock
50 mg ￥9900 In-stock
100 mg ￥14500 In-stock
200 mg   询价  
500 mg   询价  

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(1E)-CFI-400437 dihydrochloride 相关产品

•相关化合物库:

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生物活性

(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].

IC50 & Target[1]

PLK3

0.6 nM (IC50)

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 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

565.49

Formula

C29H30Cl2N6O2
CAS 号

1247000-76-5
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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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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