1505514-27-1
Chemical Structure
Taletrectinib free base
Synonym(s): DS-6051b free base; AB-106 free base; IBI-344 free base
- CAS No.: 1505514-27-1
- Formula:C23H24FN5O
- Molecular Weight:405.47
IUPAC Name: 3-(4-((R)-2-aminopropoxy)phenyl)-N-((R)-1-(3-fluorophenyl)ethyl)imidazo[1,2-b]pyridazin-6-amine
InChIKey: HEVHTYMYEMEBPX-HZPDHXFCSA-N
SMILES: C[C@@H](NC1=NN2C(C=C1)=NC=C2C3=CC=C(OC[C@H](N)C)C=C3)C4=CC=CC(F)=C4
Biological Activity: Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[1][2].
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Taletrectinib free base | Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants. | |||||||||||||||||||||
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- [1]. Katayama R, et al. The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models. Nat Commun. 2019;10(1):3604. Published 2019 Aug 9. [Content Brief]
- [2]. Fujiwara Y, et al. Safety and pharmacokinetics of DS-6051b in Japanese patients with non-small cell lung cancer harboring ROS1 fusions: a phase I study. Oncotarget. 2018;9(34):23729-23737. Published 2018 May 4. [Content Brief]
Keywords
