1. Protein Tyrosine Kinase/RTK
  2. Src
  3. DGY-06-116

DGY-06-116 

Cat. No.: HY-136605
Handling Instructions

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.

For research use only. We do not sell to patients.

DGY-06-116 Chemical Structure

DGY-06-116 Chemical Structure

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Description

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].

IC50 & Target

IC50: 3 nM (Src), 8340 nM (FGFR1)[1]

In Vitro

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].

Cell Proliferation Assay[1]

Cell Line: H1975 (nonsmall cell lung cancer, NSCLC), HCC827 (NSCLC), and MDA-MB-231 (triple negative breast cancer, TNBC) cell lines
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Induced strong growth inhibitory effects across all three cell lines with GR50 values of 0.3, 0.5, and 0.3 μM for H1975, HCC827, and MDA-MB-231, respectively.

Western Blot Analysis[1]

Cell Line: H1975 and HCC827 NSCLC cells
Concentration: 1 μM
Incubation Time: 2 hours
Result: Inhibited p-SRCY416 signaling in both H1975 and HCC827 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[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].

Animal Model: Adult C57B6 mice[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; for 3 times every 12 h
Result: Led to inhibition of p-SRCY416 at 2 and 4 h postdosing, compared to the vehicle controls.
Demonstrated SRC binding and inhibition at both 2 and 4 h postdosing compared to the vehicle controls.
Molecular Weight

597.11

Formula

C₃₂H₃₃ClN₈O₂

SMILES

O=C(NC1=C(Cl)C=CC=C1C)C(C=N2)=C(NC3=C(NC(C=C)=O)C=CC=C3)N=C2NC4=CC=C(N5CCN(C)CC5)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

DGY-06-116SrcirreversiblecovalentFGFR1lungcancerNSCLCTNBCInhibitorinhibitorinhibit

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DGY-06-116
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