DGY-06-116 是一种不可逆的共价选择性 Src 抑制剂，IC50 为 3 nM。DGY-06-116 抑制 FGFR1 的 IC50 为 8340 nM。
货号:ajcx33066
CAS:2556836-50-9
分子式:C32H33ClN8O2
分子量：597.11
溶解度:DMSO : 250 mg/mL (418.68 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM[1].

DGY-06-116 potently inhibits Src kinase activity with an IC50 of 2.6 nM at 1 h incubation[2].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[1].15a (1 μM; 2 hours) is capable of inducing potent SRC binding and inhibition of SRC signaling in NSCLC cells[1].

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[1]. DGY-06-116 exhibits a short half-life and high exposure (T1/2=1.29 h, AUC=12 746.25 min.ng/mL) following i.p. administration (5 mg/kg) in B6 mice[1].

[1]. Guangyan Du, et al. Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine. J Med Chem. 2020 Feb 27;63(4):1624-1641.
[2]. Deepak Gurbani, et al. Structure and Characterization of a Covalent Inhibitor of Src Kinase. Front Mol Biosci. 2020 May 19;7:81.