Home Immunology & Inflammation ROS1 inhibitor - Trk receptor inhibitor Taletrectinib (DS-6051b) For research use only.

Taletrectinib (DS-6051b)

Synonyms: AB-106

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

Taletrectinib (DS-6051b) Chemical Structure

CAS No. 1505515-69-4

Purity & Quality Control

Batch: S890101 DMSO]50 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.98%
99.98

Taletrectinib (DS-6051b) Related Products

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot pROS1 / ROS1 / pSHP-2 / SHP-2 / pMEK1 / MEK1 / pERK / ERK / pAKT / AKT / Actin 31399568
Growth inhibition assay Tumor Volume Cell viability 31399568
CT&MRI Tumor Volume 29805770
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04919811 Recruiting
Non Small Cell Lung Cancer
AnHeart Therapeutics Inc.
 September 1 2021 Phase 2
NCT05357820 Completed
Solid Tumor
AnHeart Therapeutics Inc.
 July 19 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 551.61 Formula

C29H34FN5O5
CAS No. 1505515-69-4 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 50 mg/mL ( (90.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Taletrectinib (DS-6051b) | Taletrectinib (DS-6051b) supplier | purchase Taletrectinib (DS-6051b) | Taletrectinib (DS-6051b) cost | Taletrectinib (DS-6051b) manufacturer | order Taletrectinib (DS-6051b) | Taletrectinib (DS-6051b) distributor