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Art. -Nr.: HY-155028

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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.

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CAS. Nr.: 2658488-68-5
Formel: C₂₈H₂₉ClN₄O₄
Molecular Weight:521.01

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (281 KB)

FGFR-IN-11 Chemical Structure

CAS. Nr.: 2658488-68-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

FGFR1

9.9 nM (IC₅₀)

FGFR2

3.1 nM (IC₅₀)

FGFR3

16 nM (IC₅₀)

FGFR4

1.8 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10000 μM Compound: I-5	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	[PMID: 37335602]
Hep 3B2	IC₅₀	52.6 nM Compound: I-5	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	[PMID: 37335602]
HT-29	IC₅₀	7233 μM Compound: I-5	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	[PMID: 37335602]
Huh-7	IC₅₀	12.63 nM Compound: I-5	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	[PMID: 37335602]
MCF7	IC₅₀	>10000 μM Compound: I-5	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	[PMID: 37335602]
MV4-11	IC₅₀	>10000 μM Compound: I-5	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	[PMID: 37335602]
NCI-H1581	IC₅₀	<0.31 μM Compound: I-5	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	[PMID: 37335602]
SNU-16	IC₅₀	1.8 μM Compound: I-5	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	[PMID: 37335602]

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

NCI-H1581, SNU16, Huh-7, Hep3B
Concentration:

0.3 nM-20 μM
Incubation Time:

72 h
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).

In Vivo

FGFR-IN-11 (60 mg/kg, p.o., QD for 21 days) inhibits tumor growth significantly and without effect on body weight in the Huh-7 or NCI-H1581 xenograft model in female nude mice^[1].
Pharmacokinetic Study of FGFR-IN-11 (compound I-5)^[1]

parameters (unit)	C₀ (ng/mL)	C_max (ng/mL)	T_1/2 (h)	T_max (h)	AUC_(0-t) (h ng/mL)	AUC_(0-∞) (h ng/mL)	MRT_(0-t) (h)	MRT_(0-∞) (h)	CI (mL/kg/min)	V_ss (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.

Animal Model:

Huh-7 xenograft model in female nude mice^[1]
Dosage:

15, 30, 60 mg/kg
Administration:

Oral administration (p.o.)
Result:

Inhibited tumor growth of 88.2% at the dose of 60 mg/kg and had no significant changes in body weight.

Animal Model:

NCI-H1581 xenograft model in female nude mice^[1]
Dosage:

60 mg/kg
Administration:

Oral administration (p.o.)
Result:

Inhibited tumor growth of 67% and had no significant changes in body weight.

Chemical Information

CAS. Nr. 2658488-68-5
Molecular Weight 521.01
Formel C₂₈H₂₉ClN₄O₄
SMILES

O=C(N1CCC(CC1)C2=CC3=C(OC4=CC=C(C(Cl)=C4)NC(NC5CC5)=O)C=CN=C3C=C2OC)C=C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hu S, et al. Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors. J Med Chem. 2023 Jul 13;66(13):8858-8875. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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