DS-6051b

Research use only, not for human use.

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 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.

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.

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Taletrectinib,AB-106

Immunology/Inflammation

ROS

ROS1| TrkA| TrkB| TrkC

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1505515-69-4

551.61

C29H34FN5O5

>98% (HPLC)

DMSO:50 mg/ml (90.64 mM)

OC(=O)CCCCC(O)=O.C[C@@H](N)COc1ccc(cc1)-c1cnc2ccc(N[C@H](C)c3cccc(F)c3)nn12

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(-20℃)

With Ice Pack

≥ 2 years