InformationTaletrectinib (DS-6051b, AB-106) is a new-generation selectiveROS1/NTRKinhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.TargetsROS1 (Cell-free assay); TrkA (Cell-free assay); TrkC (Cell-free assay); TrkB (Cell-free assay) 0.207 nM; 0.622 nM; 0.980 nM; 2.28 nMIn vitroDS-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.In vivoIn vivo experiments using the KM12-bearing mouse xenograft model shows that DS-6051b induced tumor shrinkage at a ≥50/u2009mg/kg or higher treatment dose without significant body weight loss. Specification: 10mM in DMSO Molecular Formula: C29H34FN5O5 Molecular Weight: 551.61 PubChem CID: 72694302 Isomeric SMILES: C[C@H](COC1=CC=C(C=C1)C2=CN=C3N2N=C(C=C3)N[C@H](C)C4=CC(=CC=C4)F)N.C(CCC(=O)O)CC(=O)O
- UPC:
- 51342906
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 0.85 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- T421775-1ml
- CAS:
- 1505515-69-4
- Product Size:
- 1ml
