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ASP5878

カタログ番号GC34476

ASP5878 は、FGFR 1、2、3、および 4 の経口活性阻害剤であり、FGFR 1、2、3、および 4 キナーゼ活性の IC50 値は 0.47 nM、0.6 nM、0.74 nM、および 3.5 nM です。 ASP5878 には潜在的な抗腫瘍活性があります。

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ASP5878 化学構造

Cas No.: 1453208-66-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$232.00
在庫あり
5mg
$211.00
在庫あり
10mg
$340.00
在庫あり
25mg
$680.00
在庫あり
50mg
$1,089.00
在庫あり
100mg
$1,544.00
在庫あり

Tel:(909) 407-4943 Email: sales@glpbio.com

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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]. FGFR1|0.47 nM (IC50)|FGFR2|0.6 nM (IC50)|FGFR3|0.74 nM (IC50)|FGFR4|3.5 nM (IC50)

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]. Cell Viability Assay[1] Cell Line: Human HCC cell lines.

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]. Animal Model: Four-week-old male nude mice (CAnN.Cg-Foxn1nu/CrlCrlj [nu/nu]) (Hep3B2.1-7 cells inoculated subcutaneously)[1].

[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.

Chemical Properties

Cas No. 1453208-66-6 SDF
Canonical SMILES OCCN1N=CC(NC2=NC=C(OCC3=C(F)C(OC)=CC(OC)=C3F)C=N2)=C1
Formula C18H19F2N5O4 M.Wt 407.37
溶解度 DMSO : ≥ 250 mg/mL (613.69 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4548 mL 12.2739 mL 24.5477 mL
5 mM 0.491 mL 2.4548 mL 4.9095 mL
10 mM 0.2455 mL 1.2274 mL 2.4548 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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