(1E)-CFI-400437 dihydrochloride - CAS:1247000-76-5

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(1E)-CFI-400437 dihydrochloride

目录号 : KM8358 CAS No. : 1247000-76-5

Data Sheet 产品使用指南

(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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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(1E)-CFI-400437 dihydrochloride In-stock

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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.

体内研究

(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth.
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%.

Animal Model:	6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model)
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.

分子式

C₂₉H₃₀Cl₂N₆O₂

分子量

565.49

CAS号

1247000-76-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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°C)

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 (protect from 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。