FGFR4-IN-20
FGFR4-IN-20 (comp 11) is an orally active and selective FGFR4 inhibitor with IC50s of 19 and 36 nM against Huh7 cells and FGFR4 enzyme. FGFR4-IN-20 can be used for hepatocellular carcinoma research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C26H22Cl2N4O3
- 分子量:509.38
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
FGFR4 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | GI50 |
16 nM
Compound: 11
|
Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Hep3B cells by SRB assay
Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Hep3B cells by SRB assay
|
[PMID: 38706130] |
| Hep 3B2 | IC50 |
16 nM
Compound: 11
|
Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay
Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay
|
[PMID: 38706130] |
| HepG2 | GI50 |
335 nM
Compound: 11
|
Growth inhibition of human HepG2 cells by SRB assay
Growth inhibition of human HepG2 cells by SRB assay
|
[PMID: 38706130] |
| HS27 | GI50 |
913 nM
Compound: 11
|
Growth inhibition of human HS27 cells by SRB assay
Growth inhibition of human HS27 cells by SRB assay
|
[PMID: 38706130] |
| Huh-7 | GI50 |
16 nM
Compound: 11
|
Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Huh-7 cells by SRB assay
Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Huh-7 cells by SRB assay
|
[PMID: 38706130] |
| Huh-7 | IC50 |
19 nM
Compound: 11
|
Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay
Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay
|
[PMID: 38706130] |
| PLC-PRF-5 | GI50 |
598 nM
Compound: 11
|
Growth inhibition of human PLCPRF5 cells by SRB assay
Growth inhibition of human PLCPRF5 cells by SRB assay
|
[PMID: 38706130] |
| RT-112 | GI50 |
151 nM
Compound: 11
|
Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay
Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay
|
[PMID: 38706130] |
| SNU-387 | GI50 |
251 nM
Compound: 11
|
Growth inhibition of human SNU-387 cells by SRB assay
Growth inhibition of human SNU-387 cells by SRB assay
|
[PMID: 38706130] |
FGFR4-IN-20 (0.01-1000 nM) shows IC50s of 19, 16 and 33 nM against Huh7 (FGFR4 overexpression), Hep3B (FGF19 amplification) and JHH-7 (FGF19 amplification) cell lines, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetics Profile of FGFR4-IN-20 in ICR Mice[1]
| Parameter | IV (5 mg/kg) | PO (100 mg/kg, QD) |
| AUC0-24 (ng·h/mL) | 4810 | 59534 |
| Cmax (ng/mL) | 8137 | 24566 |
| Tmax (h) | 0.5 | |
| T1/2 (h) | 1.7 | 3.9 |
| F% | 61.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 509.38
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分子式 C26H22Cl2N4O3
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SMILES
ClC1=C(C2=CC3=CN=C(C=C3C(C)=N2)NC4=C(C=CC=C4)NC(C=C)=O)C(Cl)=C(OC)C=C1OC
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)