Art. -Nr.: HY-156086

TRK-IN-24

TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA^G595R, TRKA^G667C and TRKA^F589L IC₅₀s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1^G595R and BaF3-CD74-NTRK1^G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC₅₀ of 1.43-47.56 nM.

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CAS. Nr.: 2937544-01-7
Formel: C₃₉H₄₅N₇O₃
Molecular Weight:659.82

Speicherung:

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

Data Sheet (269 KB)

TRK-IN-24 Chemical Structure

CAS. Nr.: 2937544-01-7

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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

IC50: 5.21 nM (TRKA), 4.51 nM (TRKC), 6.77 nM (TRKA^G595R), 1.42 nM (TRKA^G667C), 6.13 nM (TRKA^F589L)^[1]

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1.43 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G667C mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	1.7 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	121.09 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	17.67 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-NTRK3 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.36 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G667A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.37 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.38 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623E mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	2.46 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G696A mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	22.82 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC V601M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	25.44 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring wild type ETV6-TRKB incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	26.4 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G709C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	27.07 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G6678 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	27.2 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRK1 G595R mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	315.8 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA G595R/G667C mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	46.15 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB G639R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	47.56 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB F633L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-TRKA V573M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.12 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKB V617M mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	5.56 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G6968 mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	6.13 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring TRKA-F589L fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	6.42 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC G623R mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	7.68 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring ETV6-TRKC F617L mutant incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	8.62 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells harbouring CD74-NTRKIF 589L mutant fusion protein incubated for 3 days by CCK8 method	[PMID: 37676745]
BaF3	IC₅₀	982.75 nM Compound: 10g	Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method Antiproliferative activity against mouse BaF3 cells incubated for 3 days by CCK8 method	[PMID: 37676745]

In Vitro

TRK-IN-24 (compound 10g) (3.7-300 nM) inhibits the phosphorylation of AKT, TRKA, PLCγ1, and ERK in Ba/F3 cells^[1].

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

In Vivo

TRK-IN-24 (compound 10g) (50 mg/kg; 10-14 days) in mice BaF3-CD74-NTRK1^G595R and BaF3-CD74-NTRK1^G667C In xenograft models, treatment resulted in 72% and 78% tumor regression after 10 or 14 days, respectively^[1].

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

Chemical Information

CAS. Nr. 2937544-01-7
Molecular Weight 659.82
Formel C₃₉H₄₅N₇O₃
SMILES

CC(C(C#CC1=CN=C2C=CC3=NN21)=CC(OCCCCCCCNC3=O)=C4)=C4C(NC5=CC(C6CC6)=CC(CN7CCN(CC7)C)=C5)=O
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 (269 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]. Wang Z, et al. Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations. J Med Chem. 2023 Sep 7.. . [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.

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