MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報,，我們不為任何個人用途提供產(chǎn)品和服務(wù),。

DGY-06-116

產(chǎn)品活性：DGY-06-116 是一種不可逆的共價選擇性 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：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.

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