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Cat. No.: HY-190792

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TrkA-IN-24

TrkA-IN-24 is a potent covalent TRKA inhibitor with an IC₅₀ of 23.1 nM and a K_i of 1.48 µM against TRKA-G595R. TrkA-IN-24 overcomes the acquired resistance to Larotrectinib (HY-12866) caused by such mutations by covalently targeting and modifying the arginine residue Arg595 newly introduced by the mutation in the mutant TRKA kinase. TrkA-IN-24 can be used for research on TRKA-mutant tumors.

For research use only. We do not sell to patients.

Formula: C₂₄H₂₀F₂N₄O₃
Molecular Weight:450.44

Storage:

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

Data Sheet (288 KB)

TrkA-IN-24 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

TRKA^G595R

23.1
nM (IC₅₀)

All Trk Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI₅₀	1.82 μM	Antiproliferative activity against Ba/F3-CD74-TRKA-G595R cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against Ba/F3-CD74-TRKA-G595R cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	42911680

In Vitro

TrkA-IN-24 (compound L1a) (72 h) exhibits moderate inhibition of cell proliferation in Ba/F3-CD74-TRKA-G595R cells, with a GI₅₀ of 1.82 μM^[1].
TrkA-IN-24 potently inhibits recombinant TRKA-G595R kinase activity with an IC₅₀ of 23.1 nM and a K_i of 1.48 µM^[1].

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

Related Protocols :

Genotoxicity/Mutagenicity Study

Chemical Information

Molecular Weight 450.44
Formula C₂₄H₂₀F₂N₄O₃
SMILES

O=C(C1=CC=CC(C2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2)=C1)C(O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 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)

References

[1]. Wang Z, et al. Discovery of Arginine-Reactive Covalent Kinase Inhibitors Overcoming Clinical Drug Resistance. Journal of medicinal chemistry. 2026 Oct 22;69(20):24010-24029. [Content Brief]

Calculators

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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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MOQ

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100 mg

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