Type II TRK inhibitor 1

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Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA^G667C and ETV6-TRKC^G696C fusion proteins with IC₅₀s of 6 nM and 1.7 nM, respectively. Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Type II TRK inhibitor 1 Chemical Structure

CAS No. : 2937543-72-9

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TrkA TrkB TrkC Trk

Biological Activity
Purity & Documentation
References
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Description

Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA^G667C and ETV6-TRKC^G696C fusion proteins with IC₅₀s of 6 nM and 1.7 nM, respectively^[1]. Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

TrkA

TrkC

In Vitro

Type II TRK inhibitor 1 (compound 7b) (3.1-800 nM; 2 h) inhibits the phosphorylation of TRKA, PLCγ1, and ERK^[1].

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

Western Blot Analysis^[1]

Cell Line:	Ba/F3 engineered cells harboring CD74-TRKA, CD74-TRKA^G667C, and CD74-TRKA^G595R
Concentration:	0 nM, 3.1 nM, 12.5 nM, 50 nM, 200 nM, 800 nM
Incubation Time:	24 hours
Result:	Decreased the protein level of p-TRKA, p-PLCγ1, p-ERK in cells.

Molecular Weight

670.68

Formula

C₃₅H₃₃F₃N₈O₃

CAS No.

2937543-72-9

SMILES

CN(CCN1)C2=NN3C(C=C2)=NC=C3C#CC4=CC(OCCCCC1=O)=CC(C(NC5=CC(N6C=C(C)N=C6)=CC(C(F)(F)F)=C5)=O)=C4C

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wang Z, et al. Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance. J Med Chem. 2022 Apr 28;65(8):6325-6337. [Content Brief]