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Art. -Nr.: HY-175302

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TRK-IN-32

TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRK^WT, TRK^G595R and TRK^G667C with IC₅₀ values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKA^WT and Ba/F3-TRKA^G667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma).

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CAS. Nr.: 3044124-79-7
Formel: C₁₉H₁₈FN₇
Molecular Weight:363.39

Speicherung:

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

Data Sheet (274 KB)

TRK-IN-32 Chemical Structure

CAS. Nr.: 3044124-79-7

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

TRK-IN-32 (Compound 15m) exhibits moderate human liver microsomal stability (t_{1/2_{= 33.8 min)^[1].

TRK-IN-32 exhibits anti-proliferative efficacy against Ba/F3 cell lines, with an IC₅₀s of 1.24 (Ba/F3-ETV6-TRKA^WT), 0.35 (Ba/F3-ETV6-TRKB^WT), 24.26 (Ba/F3-LMNA-TRKA^G595R), 10.24 (Ba/F3-LMNA-TRKA^G667C) and 1.06 (Ba/F3-LMNA-TRKA^F589L) nM^[1].

TRK-IN-32 (0-10 nM) effectively blocks the TRKA^WT and TRKA^G667C autophosphorylation in cells at relatively low concentrations as well as phosphorylation of their downstream molecules AKT, PLCγ1 and ERK in Ba/F3 cells expressing TRKA^WT and TRKA^G667C fusion mutant^[1].

TRK-IN-32 (0-500 nM, 48 h) strongly induces Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells apoptosis^[1].}}

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

Apoptosis Analysis^[1]

Cell Line:

Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKAG667C cells
Concentration:

10, 50, 100, 500 nM
Incubation Time:

48 h
Result:

Observed significant apoptosis rates of 18.74% at 100 nM and 35.65% at 500 nM in Ba/F3-CD74-TRKA cells.
Induced noticeable apoptosis rates of 11.22% and 56.25%, respectively. at concentrations of 10 nM and 50 nM in Ba/F3-CD74-TRKAG667C cells.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-inf	V_d	CL	MRT_0-t	MRT_0-inf	F
Rat^[1]	10 mg/kg	p.o.	2.43 h	2.00 h	1363.33 ng/mL	5581.58 ng·h/mL	5582.96 ng·h/mL	6454.96 mL/kg	1810.18 mL/h/kg	2.77 h	2.78 h	55.26 %
Rat^[1]	2 mg/kg	i.v.	1.08 h	0.08 h	1606.67 ng/mL	2020.09 ng·h/mL	2039.54 ng·h/mL	1510.95 mL/kg	1007.89 mL/h/kg	1.36 h	1.42 h	/

Chemical Information

CAS. Nr. 3044124-79-7
Molecular Weight 363.39
Formel C₁₉H₁₈FN₇
SMILES

C[C@@H](C1=CC=C(C=N1)F)NC2=NN3C(C4=NNC(C5CC5)=C4)=CN=C3C=C2
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 (274 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]. Xu Y, et al. Discovery of imidazo[1,2-b]pyridazine derivatives as potent TRK inhibitors for overcoming multiple resistant mutants. Bioorg Chem. 2025 Aug;163:108737. [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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Biologische Aktivität
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- In Vitro
Chemical Information
Reinheit & Dokumentation
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TRK-IN-32

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

TRK-IN-32 Related Classifications

HY-175302 Related Classifications