Taletrectinib | ROS1/NTRK inhibitor | Probechem Biochemicals

Chemical Structure : Taletrectinib

CAS No.: 1505515-69-4

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Taletrectinib (DS-6051b, AB-106, IBI-344)

货号: 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).

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10 mg	￥2280	In stock
25 mg	￥3780	In stock
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生物&药学活性

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.

物理化学性质&存储条件

分子量	405.477
分子式	C23H24FN5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(4-((R)-2-aminopropoxy)phenyl)-N-((R)-1-(3-fluorophenyl)ethyl)imidazo[1,2-b]pyridazin-6-amine

参考文献

1. Katayama R, et al. Nat Commun. 2019 Aug 9;10(1):3604.

Taletrectinib (DS-6051b, AB-106, IBI-344)

生物&药学活性

物理化学性质&存储条件

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Taletrectinib (DS-6051b, AB-106, IBI-344)

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物理化学性质&存储条件

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