DGY-06-116
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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- Pureté: 98.62%
- CAS No.: 2556836-50-9
- Formule: C32H33ClN8O2
- Masse moléculaire:597.11
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) DGY-06-116
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Activité biologique
IC50: 3 nM (Src), 8340 nM (FGFR1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>2927 nM
Compound: 15a
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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
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[PMID: 31935084] |
| HCC827 | IC50 |
0.5 μM
Compound: 15a
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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
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[PMID: 31935084] |
| MDA-MB-231 | IC50 |
0.3 μM
Compound: 15a
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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
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[PMID: 31935084] |
| NCI-H1975 | IC50 |
0.3 μM
Compound: 15a
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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
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[PMID: 31935084] |
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.
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Cell Line:H1975 (nonsmall cell lung cancer, NSCLC), HCC827 (NSCLC), and MDA-MB-231 (triple negative breast cancer, TNBC) cell lines
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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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.
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Cell Line:H1975 and HCC827 NSCLC cells
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Concentration:1 μM
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Incubation Time:2 hours
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Result:Inhibited p-SRCY416 signaling in both H1975 and HCC827 cells.
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.
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Animal Model:Adult C57B6 mice[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; for 3 times every 12 h
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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.
Chemical Information
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CAS No. 2556836-50-9
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Appearance Solid
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Masse moléculaire 597.11
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Formule C32H33ClN8O2
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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
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Most Recent
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Sci Adv
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
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[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]
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 |
DGY-06-116 Related Classifications
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