Art. -Nr.: HY-136605

DGY-06-116

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

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Reinheit: 98.62%
CAS. Nr.: 2556836-50-9
Formel: C₃₂H₃₃ClN₈O₂
Molecular Weight:597.11

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

DGY-06-116 Chemical Structure

CAS. Nr.: 2556836-50-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

Alle Src Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>2927 nM Compound: 15a	Cytotoxicity against mouse BA/F3 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Cytotoxicity against mouse BA/F3 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 31935084]
HCC827	IC₅₀	0.5 μM Compound: 15a	Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 31935084]
MDA-MB-231	IC₅₀	0.3 μM Compound: 15a	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 31935084]
NCI-H1975	IC₅₀	0.3 μM Compound: 15a	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay	[PMID: 31935084]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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-SRC^Y416 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 (T_1/2=1.29 h, AUC=12 746.25 min·ng/mL) following i.p. administration (5 mg/kg) in B6 mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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-SRC^Y416 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.

Chemical Information

CAS. Nr. 2556836-50-9
Appearance Solid
Molecular Weight 597.11
Formel C₃₂H₃₃ClN₈O₂
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

Sci Adv

SRC kinase drives multidrug resistance induced by KRAS-G12C inhibition. [Abstract]

2024 Dec 13;10(50):eadq4274. PMID: 39661665
Cell Death Dis

4EBP1 senses extracellular glucose deprivation and initiates cell death signaling in lung cancer. [Abstract]

2022 Dec 27;13(12):1075. PMID: 36575176

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (418.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6747 mL

8.3737 mL

16.7473 mL

5 mM

0.3349 mL

1.6747 mL

3.3495 mL

10 mM

0.1675 mL

0.8374 mL

1.6747 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. Deepak Gurbani, et al. Structure and Characterization of a Covalent Inhibitor of Src Kinase. Front Mol Biosci. 2020 May 19;7:81. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6747 mL	8.3737 mL	16.7473 mL	41.8683 mL
	5 mM	0.3349 mL	1.6747 mL	3.3495 mL	8.3737 mL
	10 mM	0.1675 mL	0.8374 mL	1.6747 mL	4.1868 mL
	15 mM	0.1116 mL	0.5582 mL	1.1165 mL	2.7912 mL
	20 mM	0.0837 mL	0.4187 mL	0.8374 mL	2.0934 mL
	25 mM	0.0670 mL	0.3349 mL	0.6699 mL	1.6747 mL
	30 mM	0.0558 mL	0.2791 mL	0.5582 mL	1.3956 mL
	40 mM	0.0419 mL	0.2093 mL	0.4187 mL	1.0467 mL
	50 mM	0.0335 mL	0.1675 mL	0.3349 mL	0.8374 mL
	60 mM	0.0279 mL	0.1396 mL	0.2791 mL	0.6978 mL
	80 mM	0.0209 mL	0.1047 mL	0.2093 mL	0.5234 mL
	100 mM	0.0167 mL	0.0837 mL	0.1675 mL	0.4187 mL

Keywords

DGY-06-116

2 Cited Publications

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DGY-06-116

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

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) DGY-06-116

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DGY-06-116

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

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) DGY-06-116

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DGY-06-116 Related Classifications

HY-136605 Related Classifications