Zurletrectinib

Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM) . Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations) . Zurletrectinib can be used for the study of glioma[1].

Product Specifications

CAS Number

[2403703-30-8]

Product Name Alternative

ICP-723

UNSPSC

12352005

Target

C-Met/HGFR; Trk Receptor

Type

Reference compound

Related Pathways

Neuronal Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/zurletrectinib.html

Purity

99.32

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1NC2=C3N=C(N4[C@@](C[C@@](F)([H])C4)([H])C5=CC(F)=CN=C5O[C@](C)([H])CN1)C=CN3N=C2

Molecular Formula

C19H19F2N7O2

Molecular Weight

415.40

References & Citations

[1]Kong NX, et al. Preparation of the heterocyclic compounds as trk inhibitor: World Intellectual Property Organization, WO2020001415. 2020-01-02.|[2]WHO Drug Information-World Health Organization (WHO) .|[3]Roa P, et al. Zurletrectinib is a next-generation TRK inhibitor with strong intracranial activity against NTRK fusion-positive tumours with on-target resistance to first-generation agents. Br J Cancer. 2024 Aug;131 (3) :601-610.