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Taletrectinib (free base)

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

Product Specifications

CAS Number

1505514-27-1

Product Name Alternative

DS-6051b (free base) ; AB-106 (free base) ; IBI-344 (free base)

UNSPSC

12352005

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-free-base.html

Solubility

10 mM in DMSO

Smiles

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

C23H24FN5O

Molecular Weight

405.47

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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 3

Frequently Asked Questions

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