FGFR-IN-9
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4WT, FGFR3, FGFR4V550L, FGFR2 and FGFR1, respectively.
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- CAS 番号: 3024090-08-9
- 分子式: C25H28N6O3S
- 分子量:492.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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FGFR4WT 17.1 nM (IC50) |
FGFR3 29.6 nM (IC50) |
FGFR4V550L 30.7 nM (IC50) |
FGFR2 46.7 nM (IC50) |
FGFR1 64.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
260 nM
Compound: 19
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Cytotoxicity against mouse BaF3 cells expressing TEL-fused FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing TEL-fused FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 36480917] |
| BaF3 | IC50 |
82.5 nM
Compound: 19
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Cytotoxicity against mouse BaF3 cells expressing wild type TEL-fused FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse BaF3 cells expressing wild type TEL-fused FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 36480917] |
| BaF3 | IC50 |
>2000 nM
Compound: 19
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Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 36480917] |
| Huh-7 | IC50 |
94.7 nM
Compound: 19
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Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 36480917] |
| KATO III stomach cancer cell line | IC50 |
6 nM
Compound: 19
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Cytotoxicity against FGFR2-amplified human KATO III stomach cancer cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Cytotoxicity against FGFR2-amplified human KATO III stomach cancer cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 36480917] |
| NCI-H1581 | IC50 |
24.6 nM
Compound: 19
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Cytotoxicity against FGFR1-amplified human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Cytotoxicity against FGFR1-amplified human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 36480917] |
FGFR-IN-9 (Compound 19) (0-2 mM; 72 h) inhibits HUH7 cells with an IC50 of 94.7 ± 28.6 nM, and inhibits proliferation with IC50s of 82.5 ± 19.2 nM and 260.0 ± 50.2 nM against Ba/F3 FGFR4WT and Ba/F3 FGFR4V550L cells, respectively[1].
FGFR-IN-9 (0-400 nM; 4 h) inhibits FGFR signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3-TEL-FGFR4 cells
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Concentration:0, 50, 100, 200 and 400 nM
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Incubation Time:4 h
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Result:Showed dose-dependent inhibition of the FGFR4 signal cassette, including the phosphorylation of FGFR4 and its downstream effectors FRS2 and PLCγ.
In Vivo Pharmacokinetic Profile Data for FGFR-IN-9 (Compound 19) [1]
| FGFR-IN-9 | i.v. 1 mg/kg | p.o. 10 mg/kg |
| T1/2 (h) | 1.3 | 2.37 |
| Tmax (h) | / | 2 |
| Cmax (ng/mL) | / | 202 |
| AUCmax (h·ng/mL) | 175 | 965 |
| AUCINF (h·ng/mL) | 177 | 1087 |
| MRTinf (h) | 1.13 | 3.87 |
| F (%) | / | 61.5 |
| VSS (L/kg) | 6.37 | / |
| CL (L/h/kg) | 5.65 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice, HUH7 xenograft model[1]
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Dosage:30 and 45 mg/kg
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Administration:Intragastric gavage; daily for 3 weeks
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Result:Resulted in significant tumor growth inhibition with a TGI value of 81% and an IR value of 63% at a dose of 45 mg/kg. No significant body weight loss (<5%) was observed.
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Animal Model:Male CD-1 mice[1]
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Dosage:1 mg/kg and 10 mg/kg
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Administration:i.v. and p.o. (Pharmacokinetic Analysis)
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Result:Showed good in vivo pharmacokinetic profile.
化学情報
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CAS 番号 3024090-08-9
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分子量 492.59
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分子式 C25H28N6O3S
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SMILES
O=S(N1C=CC2=CN=C(NC3=CC=C(N4C[C@H](C)N[C@H](C)C4)C=C3)N=C21)(C5=CC=CC(OC)=C5)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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)
FGFR-IN-9 関連分類
HY-152104 関連分類
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