Taletrectinib (DS-6051b)

For research use only.

Catalog No.S8901 Synonyms: AB-106

1 publication

Taletrectinib (DS-6051b) Chemical Structure

CAS No. 1505515-69-4

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.

Selleck's Taletrectinib (DS-6051b) has been cited by 1 publication

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; 

PubMed: 31399568     


Inhibition of phosphorylation of ROS1 and downstream growth signaling-related molecules by ROS1 inhibitors in Ba/F3-CD74-ROS1-G2032R cells. The cells were treated with increasing concentrations of DS-6051b or crizotinib for 2 h. The cell lysates were immunoblotted to detect the indicated proteins.

31399568
Growth inhibition assay
Cell viability; 

PubMed: 31399568     


Sensitivity of TPM3-NTRK1-induced Ba/F3 cells (a) and KM12 (b) to DS-6051b, crizotinib, lorlatinib, or alectinib. The cells were treated with a range of inhibitor doses for 72 h. Cell viability was assessed using CellTiter-Glo assay.

Tumor Volume; 

PubMed: 31399568     


BaF3-CD74-ROS1-WT (c) or -G2032R (d) cells were subcutaneously implanted into Balb-c nu/nu mice. DS-6051b (3, 10, 30, and 100 mg/kg), crizotinib (100 mg/kg), or vehicle was treated once daily by oral gavage for 4 days. The results in (c) and (d) are indicated as mean ± SE of the tumor volume of each group (N =6); parametric Dunnett’s test was conducted between the DS-6051b-treated groups and the vehicle-treated control group.

31399568
CT&MRI
Tumor Volume; 

PubMed: 29805770     


Computed tomography (CT) and magnetic resonance images (MRI) for objective responses. (A) Patient #02: 400 mg QD, 43-year-old female, ROS1 + non-small cell lung cancer (NSCLC). Best response: partial response, crizotinib treatment-naïve. This patient showed a partial response from day 43 (showing a best response of −100% from day 127). (B) Patient #09: 400 mg QD, 61-year-old female, ROS1 + NSCLC. Best response: partial response, crizotinib treatment-naïve.

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

Solubility (25°C)

In vitro DMSO 50 mg/mL (90.64 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 551.61
Formula

C29H34FN5O5

CAS No. 1505515-69-4
Storage powder
in 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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04919811 Not yet recruiting Drug: Taletrectinib Non Small Cell Lung Cancer AnHeart Therapeutics Inc. June 2021 Phase 2

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID