(1E)-CFI-400437 dihydrochloride|cas:1247000-76-5|西域试剂

(1E)-CFI-400437 dihydrochloride,98.89%

产品编号：Bellancom-132135| CAS NO：1247000-76-5| 分子式：C₂₉H₃₀Cl₂N₆O₂| 分子量：565.49

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-132135	￥2100.00	杭州北京（现货）
Bellancom-132135	￥3200.00	杭州北京（现货）
Bellancom-132135	￥6500.00	杭州北京（现货）
Bellancom-132135	￥9900.00	杭州北京（现货）
Bellancom-132135	￥14500.00	杭州北京（现货）

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(1E)-CFI-400437 dihydrochloride

产品介绍

(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 AuroraA、 AuroraB、 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 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.

体外研究

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%.

西域 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)
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.

体内研究

西域 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)
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.

性状

Solid

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 (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。

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)

参考文献