DS-6051b

SKU: orb1219684

Description

DS-6051b is a new-generation selective inhibitor of ROS1/NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.DS-6051b inhibited the growth of the ROS1 fusion-positive HCC78 cancer cell line and the CD74-ROS1 overexpressed Ba/F3 cells. DS-6051b potently inhibited autophosphorylation of ROS1 in the SLC34A2-ROS1 harboring HCC78 cells and CD74-ROS1-expressed Ba/F3 cells at approximately single-digit to double-digit nanomolar concentration.DS-6051b induced tumor shrinkage at a ≥50mg/kg in vivo experiments using the KM12-bearing mouse xenograft model or higher treatment dose without significant body weight loss.

Key Properties

• CAS Number: 1505515-69-4
• MW: 551.61
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₄FN₅O₅
• SMILES: OC(=O)CCCCC(O)=O.C[C@@H](N)COc1ccc(cc1)-c1cnc2ccc(N[C@H](C)c3cccc(F)c3)nn12
• Target: ROS
• Solubility: DMSO:50 mg/ml (90.64 mM)

Bioactivity

• In Vitro:
  Cell Viability Assay Cell line: TPM3-NTRK1-induced Ba/F3 cells, KM12 cells. Concentration: 1-1000 nM. Incubation time: 72 hours. Result: Inhibited TPM3-NTRK1-induced Ba/F3 cells and KM12 cells viability. Western blot analysis. Cell line: U-118 MG cells (harboring FIG-ROS1 fusion gene). Concentration: 0.001-1000 nM Incubation time: 2 hours. Result: Dose dependently inhibited autophosphorylation of ROS1 in U-118-MG cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Taletrectinib,AB-106

Quick Database Links

Gene Symbol

ROS