Taletrectinib (DS-6051b)

Catalog No.S8901 Synonyms: AB-106

For research use only.

Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.

Taletrectinib (DS-6051b) Chemical Structure

CAS No. 1505515-69-4

Selleck's Taletrectinib (DS-6051b) has been cited by 2 Publications

Purity & Quality Control

Choose Selective ROS1 Inhibitors

Biological Activity

Description Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.
Targets
ROS1 [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
TrkC [1]
(Cell-free assay)
TrkB [1]
(Cell-free assay)
0.207 nM 0.622 nM 0.980 nM 2.28 nM
In vitro

DS-6051b inhibited the growth of the CD74-ROS1 overexpressed Ba/F3 cells and the ROS1 fusion-positive HCC78 cancer cell line.DS-6051b potently inhibited autophosphorylation of ROS1 in CD74-ROS1–expressed Ba/F3 cells and the SLC34A2-ROS1 harboring HCC78 cells at approximately single-digit to double-digit nanomolar concentration.[1]

Assay
Methods Test Index PMID
Western blot pROS1 / ROS1 / pSHP-2 / SHP-2 / pMEK1 / MEK1 / pERK / ERK / pAKT / AKT / Actin 31399568
Growth inhibition assay Cell viability ; Tumor Volume 31399568
CT&MRI Tumor Volume 29805770
In vivo

In vivo experiments using the KM12-bearing mouse xenograft model shows that DS-6051b induced tumor shrinkage at a ≥50 mg/kg or higher treatment dose without significant body weight loss.[1]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 551.61
Formula

C29H34FN5O5

CAS No. 1505515-69-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(COC1=CC=C(C=C1)C2=CN=C3N2N=C(C=C3)NC(C)C4=CC(=CC=C4)F)N.C(CCC(=O)O)CC(=O)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04919811 Recruiting Drug: Taletrectinib Non Small Cell Lung Cancer AnHeart Therapeutics Inc. September 1 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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