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Art. -Nr.: HY-151903S

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FGFR2/3-IN-1

FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC₅₀s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC₅₀s of 2.7 nM and 6.1 nM, respectively.

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CAS. Nr.: 2640352-86-7
Formel: C₂₃H₂₂D₃N₇O₃
Molecular Weight:450.51

Speicherung:

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

Data Sheet (275 KB)

FGFR2/3-IN-1 Chemical Structure

CAS. Nr.: 2640352-86-7

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Preis

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

FGFR2

1 nM (IC₅₀)

FGFR3

0.5 nM (IC₅₀)

FGFR3 V555L

2.7 nM (IC₅₀)

FGFR3 V555M

6.1 nM (IC₅₀)

FGFR1

21 nM (IC₅₀)

FGFR4

145 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	0.5 nM Compound: 29	Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition a Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition a	[PMID: 36356320]
Sf9	IC₅₀	1 nM Compound: 29	Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and m Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and m	[PMID: 36356320]

In Vitro

FGFR2/3-IN-1 (compound 29) has a clean CYP profile (CYP3A4 IC50 >25 μM). FGFR2/3-IN-1 displays excellent potency (whole blood, IC50 = 177 nM) in a whole blood (WB) assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .

In Vivo

FGFR2/3-IN-1 (compound 29) is advanced into rat pharmacokinetics studies. Clearance in the i.v. arm is low (hepatic blood flow (HBF) = 35%), with a moderate half-life (t_1/2 = 1.7 h). In the p.o. dose, FGFR2/3-IN-1 demonstrates good exposure (AUC = 5108 nM·h) and high oral bioavailability (F% = 82)^[2].

rat i.v.		rat p.o.
dose (mg/kg)	1.0	dose (mg/kg)	3.0
HBF%	35	C_max (nM)	2303
V_dss (L/kg)	1.6	AUC (nM·h)	5108
T_1/2 (h)	1.7	F%	82

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Anwendung

1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

Chemical Information

CAS. Nr. 2640352-86-7
Molecular Weight 450.51
Formel C₂₃H₂₂D₃N₇O₃
SMILES

[2H]C([2H])(NC(C1=CC(C2=C3N=C(C(C4=CN(N=C4)C(C)C)=CN3N=C2)O[C@@H]5COCC5)=CN=C1)=O)[2H]
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 (275 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]. Artem Shvartsbart, et al. Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3. J Med Chem. 2022 Nov 24;65(22):15433-15442. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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