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CAS | 2097002-61-2 | 纯度 | 99.90% |
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分子量 | 380.42 | 分子式 | C₂₀H₂₁FN₆O |
供货周期 | 现货 | 规格 | 10 mg |
货号 | HY-101977 | 应用领域 | 医疗卫生,化工,生物产业,制药 |
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CAS No. : 2097002-61-2
产品活性:Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor, with IC50s of 0.6 nM and <2.5 nM for TRKA and TRKC, respectively.
研究领域:Neuronal Signaling | Protein Tyrosine Kinase/RTK
作用靶点:Trk Receptor
In Vitro: Selitrectinib (LOXO-195) demonstrates strong binding to the wild-type TRKA, TRKB and TRKC kinase domains. Selitrectinib (LOXO-195) has potent (IC50<1 nM) inhibitory activity in kinase enzyme assays. Importantly, Selitrectinib (LOXO-195) achieves low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, with IC50s ranging from 2.0-9.8 nM. 228 individual kinases in vitro are profiled at a Selitrectinib (LOXO-195) concentration of 1 μM, which is ~1667-fold higher than its IC50 for TRKA (0.6 nM). Selitrectinib (LOXO-195) is more than 1000-fold selective for 98% of non-TRK kinases tested. Selitrectinib (LOXO-195) demonstrates potent inhibition of cell proliferation in TRK fusion-containing KM12, CUTO-3, and MO-91 cell lines (IC50≤5 nM).
In Vivo: Stably transfected NIH-3T3 ΔTRKA and ΔTRKA-G595R cells are implanted subcutaneously into the flanks of nude mice. Both larotrectinib and Selitrectinib (LOXO-195) are effective at reducing phosphorylated TRKA in tumors driven by ΔTRKA. In contrast, only Selitrectinib (LOXO-195) strongly suppresses phospho-TRKA in ΔTRKA-G595R cells in a dose-dependent manner. Selitrectinib (LOXO-195) also causes inhibition of tumor growth relative to vehicle at all doses in four TRKA-dependent tumor models (ΔTRKA, ΔTRKA-G595R, ΔTRKAG667C, and TPM3-NTRK1 fusion-positive KM12 colorectal cancer cells. Larotrectinib inhibits KM12 and NIH 3T3-ΔTRKA tumors to a similar degree. Group mean body weight loss does not exceed 5% for any agent. Selitrectinib (LOXO-195) displays high selectivity for the TRK proteins
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Kinase Inhibitor Library | Neuronal Signaling Compound Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | DS-1205b free base | LM22B-10 | TRK-IN-16 | ANA-12 | PF-06733804 | Larotrectinib sulfate | Trk-IN-10 | AZ-23 | GNF-8625 monopyridin-N-piperazine hydrochloride | Trk-IN-7 | Bedinvetmab | TrkA-IN-1 | PF-6683324 | Cyclotraxin B | PF-06737007 | TRK-IN-21 | Sacibertinib | ENT-C225 | Entrectinib | Amitriptyline-d6 (hydrochloride) | Pan-Trk-IN-2 | Pan-Trk-IN-3 | Trk-IN-6 | Trk-IN-20 | GNF-5837 | TRK-IN-19 | TrkA-IN-4 | K-252a
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