FGFR-IN-11
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models.
For research use only. We do not sell to patients.
- CAS No.: 2658488-68-5
- Formula: C28H29ClN4O4
- Molecular Weight:521.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FGFR1 9.9 nM (IC50) |
FGFR2 3.1 nM (IC50) |
FGFR3 16 nM (IC50) |
FGFR4 1.8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>10000 μM
Compound: I-5
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Antiproliferative activity against human A549 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human A549 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| Hep 3B2 | IC50 |
52.6 nM
Compound: I-5
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Antiproliferative activity against human Hep3B cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human Hep3B cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| HT-29 | IC50 |
7233 μM
Compound: I-5
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Antiproliferative activity against human HT-29 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human HT-29 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| Huh-7 | IC50 |
12.63 nM
Compound: I-5
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Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human Huh-7 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| MCF7 | IC50 |
>10000 μM
Compound: I-5
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Antiproliferative activity against human MCF7 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| MV4-11 | IC50 |
>10000 μM
Compound: I-5
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Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| NCI-H1581 | IC50 |
<0.31 μM
Compound: I-5
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Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human NCI-H1581 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
| SNU-16 | IC50 |
1.8 μM
Compound: I-5
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Antiproliferative activity against human SNU-16 cells incubated for 72 hrs by Cell counting kit 8 method
Antiproliferative activity against human SNU-16 cells incubated for 72 hrs by Cell counting kit 8 method
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[PMID: 37335602] |
FGFR-IN-11 (0.3 nM-20 μM, 72 h) inhibits multiple cancer cell growth with nanomolar activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H1581, SNU16, Huh-7, Hep3B
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Concentration:0.3 nM-20 μM
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Incubation Time:72 h
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Result:Inhibited cell growth with IC50 values of less than 2 nM (NCI-H1581 and SNU16), 15.63 nM (Huh-7) and 52.6 nM (Hep3B).
Pharmacokinetic Study of FGFR-IN-11 (compound I-5)[1]
| parameters (unit) | C0 (ng/mL) | Cmax (ng/mL) | T1/2 (h) | Tmax (h) | AUC(0-t) (h ng/mL) | AUC(0-∞) (h ng/mL) | MRT(0-t) (h) | MRT(0-∞) (h) | CI (mL/kg/min) | Vss (mL/kg) | F (%) |
| iv (2 mg/kg) | 3295 | 1836 | 0.26 | 0.08 | 570 | 572 | 0.18 | 0.19 | 58 | 1319 | / |
| po (10 mg/kg) | / | 1802 | 2.48 | 0.25 | 1731 | 1966 | 1.99 | 3.16 | / | / | 60.69 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Huh-7 xenograft model in female nude mice[1]
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Dosage:15, 30, 60 mg/kg
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Administration:Oral administration (p.o.)
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Result:Inhibited tumor growth of 88.2% at the dose of 60 mg/kg and had no significant changes in body weight.
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Animal Model:NCI-H1581 xenograft model in female nude mice[1]
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Dosage:60 mg/kg
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Administration:Oral administration (p.o.)
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Result:Inhibited tumor growth of 67% and had no significant changes in body weight.
Chemical Information
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CAS No. 2658488-68-5
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Molecular Weight 521.01
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Formula C28H29ClN4O4
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SMILES
O=C(N1CCC(CC1)C2=CC3=C(OC4=CC=C(C(Cl)=C4)NC(NC5CC5)=O)C=CN=C3C=C2OC)C=C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FGFR-IN-11 Related Classifications
HY-155028 Related Classifications
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