DGY-06-116 |
| Katalog-Nr.GC62107 |
DGY-06-116 ist ein irreversibler, kovalenter, selektiver Src-Inhibitor mit einem IC50 von 3 nM. DGY-06-116 hemmt FGFR1 mit einem IC50 von 8340 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2556836-50-9
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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