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Taletrectinib (DS-6051b) ROS1 inhibitor

Name: Taletrectinib (DS-6051b)
Brand: Selleck Chemicals
SKU: S8901
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8901

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

Chemical Structure

Molecular Weight: 551.61

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.98

Related Targets	Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor TNF-alpha ROS Parasite PD-1/PD-L1 TLR Prostaglandin Receptor IFN CXCR Nrf2 NOS CCR NLRP3 eIF STING AhR IL Receptor NADPH-oxidase Complement System IRAK β-lactamase IDO/TDO PGES FKBP
Related Products	Zidesamtinib

Chemical Information, Storage & Stability

Molecular Weight	551.61	Formula	C₂₉H₃₄FN₅O₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1505515-69-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AB-106			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

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (90.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	10% DMSO 1 40% PEG 300 2 5%Tween80 3 45%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.06mM)	Taking the 1 mL working solution as an example, add 100 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	ROS1 ^[1] (Cell-free assay) 0.207 nM TrkA ^[1] (Cell-free assay) 0.622 nM TrkC ^[1] (Cell-free assay) 0.980 nM TrkB ^[1] (Cell-free assay) 2.28 nM
In vitro	Taletrectinib (DS-6051b) inhibited the growth of the CD74-ROS1 overexpressed Ba/F3 cells and the ROS1 fusion-positive HCC78 cancer cell line. It 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]
In vivo	In vivo experiments using the KM12-bearing mouse xenograft model shows that Taletrectinib (DS-6051b) induced tumor shrinkage at a ≥50 mg/kg or higher treatment dose without significant body weight loss.^[1]
References	[1] https://www.ncbi.nlm.nih.gov/pubmed/?term=The+new-generation+selective+ROS1%2FNTRK+inhibitor

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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