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DGY-06-116

產(chǎn)品活性：DGY-06-116 是一種不可逆的共價(jià)選擇性 Src 抑制劑，IC₅₀ 為 3 nM。DGY-06-116 抑制 FGFR1 的 IC₅₀ 為 8340 nM。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK

作用靶點(diǎn)：Src

In Vitro: DGY-06-116 potently inhibits Src kinase activity with an IC₅₀ of 2.6 nM at 1 h incubation.
DGY-06-116 (Compound 15a; 0.01-10 μM; 72 hours) exhibits potent antiproliferative effects in nonsmall cell lung cancer (NSCLC) and triple negative breast cancer (TNBC) cell lines harboring SRC activation.
15a (1 μM; 2 hours) is capable of inducing potent SRC binding and inhibition of SRC signaling in NSCLC cells.

In Vivo: DGY-06-116 (Compound 15a; 5 mg/kg for 3 times every 12 h via intraperitoneal injection) is able to inhibit SRC for an extended duration in adult C57B6 mice, likely due to its ability to covalently bind the target.
DGY-06-116 exhibits a short half-life and high exposure (T_1/2=1.29 h, AUC=12 746.25 min·ng/mL) following i.p. administration (5 mg/kg) in B6 mice.

相關(guān)產(chǎn)品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Membrane Protein-targeted Compound Library  |  Tirbanibulin dihydrochloride  |  HIV-IN-6  |  Bafetinib  |  Multi-kinase-IN-2  |  PP2  |  PP58  |  ENMD-2076 Tartrate  |  Lck-IN-1  |  Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH  |  Ponatinib hydrochloride  |  TL02-59 dihydrochloride  |  A-770041  |  Masitinib  |  TX-1123  |  Bosutinib hydrate  |  Ponatinib-d₈  |  1-NM-PP1  |  MNS  |  TG 100801  |  Scutellarein  |  RR-SRC  |  TG 100572  |  AMG-47a  |  AD57  |  AD80  |  Dasatinib monohydrate  |  Lck Inhibitor  |  Damnacanthal

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