Taletrectinib

Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].

Product Specifications

CAS Number

[1505515-69-4]

Product Name Alternative

DS-6051b; AB-106; IBI-344

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

ROS Kinase

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

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

Purity

99.78

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(O)CCCCC(O)=O.C[C@@H](NC1=NN2C(C=C1)=NC=C2C3=CC=C(OC[C@H](N)C)C=C3)C4=CC=CC(F)=C4

Molecular Formula

C29H34FN5O5

Molecular Weight

551.61

Precautions

H302, H315, H319, H335

References & Citations

[1]Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10 (1) :3604. Published 2019 Aug 9.|[2]Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9 (34) :23729-23737. Published 2018 May 4.