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

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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DGY-06-116 Chemical Structure

DGY-06-116 Chemical Structure

CAS No. : 2556836-50-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

DGY-06-116 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DGY-06-116

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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].

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

DGY-06-116 Related Antibodies

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].

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-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
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6747 mL 8.3737 mL 16.7473 mL
5 mM 0.3349 mL 1.6747 mL 3.3495 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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DGY-06-116 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DGY-06-1162556836-50-9SrcirreversiblecovalentselectiveFGFR1Inhibitorinhibitorinhibit

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