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: 1505515-69-4

Selleck's Taletrectinib (DS-6051b) has been cited by 3 publications

Purity & Quality Control

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

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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 Cell viability Tumor Volume 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


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In vivo
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