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Chemical Structure : Taletrectinib
CAS No.: 1505515-69-4
Catalog No.: PC-73061Not For Human Use, Lab Use Only.
DS-6051b (Taletrectinib, DS 6051b) is a new-generation selective ROS1/NTRK inhibitor, potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in ATP-competitive manner (IC50=1-10 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $368 | In stock | |
| 50 mg | $798 | In stock | |
| 100 mg | $1280 | In stock | |
| 1 g | Get quote |
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DS-6051b (Taletrectinib, DS 6051b) is a new-generation selective ROS1/NTRK inhibitor, potently inhibits recombinant ROS1, NTRK1, and NTRK3 in sub-nanomolar concentration in ATP-competitive manner (IC50=1-10 nM).
DS-6051b completely inhibits ACK, ALK, DDR1, and LTK at 0.2 μM among 160 kinases in the presence of 1 mM ATP, but not other 152 kinases.
DS-6051b inhibits the growth of the CD74-ROS1 overexpressed Ba/F3 cells and the ROS1 fusion-positive HCC78 cancer cell line with a lower IC50 than crizotinib.
DS-6051b shows activity against NTRK1-TKI-resistant mutants including G595R (IC50<100 nM), effectively inhibits crizotinib-resistant ROS1 secondary mutations, including G2032R.
DS-6051b demonstrates efficacy in ROS1- or NTRK-rearranged cancer in preclinical models, including crizotinib-resistant ROS1 positive cancer with secondary kinase domain mutations especially G2032R mutation.
| M.Wt | 405.477 | |
| Formula | C23H24FN5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(4-((R)-2-aminopropoxy)phenyl)-N-((R)-1-(3-fluorophenyl)ethyl)imidazo[1,2-b]pyridazin-6-amine |
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1. Katayama R, et al. Nat Commun. 2019 Aug 9;10(1):3604.
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