FGFR4-IN-5|cas:1628793-01-0|西域试剂

FGFR4-IN-5,98.06%

产品编号：Bellancom-131704| CAS NO：1628793-01-0| 分子式：C₂₃H₂₃Cl₂N₅O₅| 分子量：520.37

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	包装	价格	库存与货期	购买量	操作
Bellancom-131704		￥4500.00	杭州北京（现货）
Bellancom-131704		￥7200.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

FGFR4-IN-5

产品介绍

FGFR4-IN-5 是一种有效的选择性共价 FGFR4 抑制剂，IC₅₀ 为 6.5 nM。FGFR4-IN-5 具有较强的抗肿瘤活性，可用于肝癌研究。

生物活性

FGFR4-IN-5 is a potent and selective covalent FGFR4 inhibitor with an IC₅₀ of 6.5 nM. FGFR4-IN-5 exhibits strong anti-tumor activity in vivo and can be used for hepatocellular carcinoma research.

体外研究

体内研究

FGFR4-IN-5 (oral gavage; 10 mg/kg; single dose) reveals a high C_max, low clearance, the C_max values are 423 ng/ml, 588 ng/ml, and 2820 ng/ml in mice, rat and cynamolgus monkey, respectively. And the oral bioavailability are 20, 12, and 27% in mouse, rat, and cyno, respectively.
FGFR4-IN-5 (oral gavage; 100 mg/kg; twice daily; 28 days) exhibits strong antitumor activity in an orthotopic Hep3B HTX model.
FGFR4-IN-5 (oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days) results in dose-dependent growth inhibition of resistant tumors. Tumor regression is observed at 30 and 100 mg/kg, with %ΔT/ΔC of 67% and 70%, respectively. However, treatment with sorafenib at 100 mg/kg once daily does not provide any benefit in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B cell bearing mice model
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg; twice daily; 28 days
Result:	Resulted in tumor regression and sustained growth inhibition.

Animal Model:	Sorafenib-resistant tumors established to mice bearing Huh7 tumors
Dosage:	10, 30, and 100 mg/kg
Administration:	Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result:	Resulted in dose-dependent growth inhibition of resistant tumors.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B cell bearing mice model
Dosage:	100 mg/kg
Administration:	Oral gavage; 100 mg/kg; twice daily; 28 days
Result:	Resulted in tumor regression and sustained growth inhibition.

Animal Model:	Sorafenib-resistant tumors established to mice bearing Huh7 tumors
Dosage:	10, 30, and 100 mg/kg
Administration:	Oral gavage; 10, 30, and 100 mg/kg; twice daily; 11 days
Result:	Resulted in dose-dependent growth inhibition of resistant tumors.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (192.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9217 mL	9.6085 mL	19.2171 mL
5 mM	0.3843 mL	1.9217 mL	3.8434 mL
10 mM	0.1922 mL	0.9609 mL	1.9217 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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。