ASP5878

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ASP5878  纯度: 99.86%

ASP5878 是具有口服活性的、FGFR 1、2、3、和 4 的抑制剂，其对FGFR 1、2、3、和 4 激酶的 IC50 值分别为 0.47 nM、0.6 nM、0.74 nM 和 3.5 nM。ASP5878 具有潜在的抗肿瘤活性。

ASP5878

ASP5878 Chemical Structure

CAS No. : 1453208-66-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
25 mg ￥9500 In-stock
50 mg ￥14500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

ASP5878 is an oral active inhibitor of FGFR 1, 2, 3, and 4, with IC50 values of 0.47 nM, 0.6 nM, 0.74 nM and 3.5 nM for FGFR 1, 2, 3, and 4 kinase activity. ASP5878 has potential antineoplastic activity[1].

IC50 & Target

FGFR1

0.47 nM (IC50)

FGFR2

0.6 nM (IC50)

FGFR3

0.74 nM (IC50)

FGFR4

3.5 nM (IC50)

体外研究
(In Vitro)

ASP5878 shows potent antiproliferative activity in most human HCC cell lines[1].
ASP5878 inhibits FGFR4 phosphorylation in a concentration-dependent manner. ASP5878 treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation[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.

Cell Viability Assay[1]

Cell Line: Human HCC cell lines.
Concentration: 0-1000 nM.
Incubation Time: 5 days.
Result: HuH-7, Hep3B2.1-7, and JHH-7 cell lines exhibited potent sensitivity to ASP5878, with IC50 values of 27, 8.5, and 21 nmol/L, respectively.
The growth inhibition rate of HLF was 64% and those of other ASP5878-sensitive cell lines were higher than 95% at 1000 nM.

体内研究
(In Vivo)

ASP5878 (3 mg/kg, orally, once daily) shows antitumor activity in a Hep3B2.1-7 subcutaneous xenograft and HCC orthotopic xenograft mouse model[1].
ASP5878 induces shrinkage of FGF19-expressing HCC xenograft model[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: Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously)[1].
Dosage: 3 mg/kg.
Administration: Orally once daily from days 14 to 52.
Result: Induced tumor regression by 9% and 88% at 1 and 3 mg/kg, respectively, without affecting the body weight for 14 days.
Induced the suppression of FGFR4 phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
Animal Model: HCC orthotopic xenograft model (mouse)[1].
Dosage: 3 mg/kg.
Administration: Orally once daily for 24 days.
Result: Exhibited a lower tumor burden than vehicle- and sorafenibtreated mice.
Induced sustained tumor regression without tumor regrowth.

Clinical Trial

分子量

407.37

Formula

C18H19F2N5O4
CAS 号

1453208-66-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 250 mg/mL (613.69 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4548 mL 12.2739 mL 24.5477 mL
5 mM 0.4910 mL 2.4548 mL 4.9095 mL
10 mM 0.2455 mL 1.2274 mL 2.4548 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.11 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.11 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Futami T, et al. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma. Mol Cancer Ther. 2017 Jan;16(1):68-75.

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