GDC-0879
Based on 4 publication(s) in Google Scholar
GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
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- Pureza: 99.49%
- No. CAS: 905281-76-7
- Fòrmula: C19H18N4O2
- Peso molecular:334.37
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) GDC-0879
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Microbiological Assay
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WB
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WB
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Flow Cytometry
Actividad biológica
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B-Raf 0.13 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A-375 | EC50 |
>500 nM
Compound: 3; GDC-0879
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Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 96 hrs by CellTiter-Glo assay
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 96 hrs by CellTiter-Glo assay
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[PMID: 29461827] |
| A-375 | IC50 |
<0.5 μM
Compound: 25, GDC-0879
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Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras
Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras
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[PMID: 22808911] |
| A-375 | IC50 |
<1 μM
Compound: 25, GDC-0879
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Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK
Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK
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[PMID: 22808911] |
| HCT-116 | IC50 |
>20 μM
Compound: 25, GDC-0879
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Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant
Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant
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[PMID: 22808911] |
GDC-0879 also inhibits pERK with an IC50 of 63 nM[1]. GDC-0879 represents a novel potent and selective B-Raf inhibitor that is being evaluated as a potential antitumor agent. GDC-0879 exhibits potent inhibition of Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines with low cellular pMEK1 inhibition IC50 estimates of 59 and 29 nM in A375 melanoma and Colo205 colorectal carcinoma cells, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 905281-76-7
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Appearance Solid
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Peso molecular 334.37
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Fòrmula C19H18N4O2
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Color White to light brown
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SMILES
O/N=C1C(C=CC(C2=CN(CCO)N=C2C3=CC=NC=C3)=C4)=C4CC/1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (4)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
BRAF inhibitors enhance erythropoiesis and treat anemia through paradoxical activation of MAPK signaling. [Abstract]2024 Dec 2;9(1):338. PMID: 39617757
GDC-0879 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]
BRAF inhibitors promoted the self-renewal of primary erythroid progenitors in vitro. The drug dose-response assay for UCB-CD34+-derived erythroid culture was conducted, with total cell numbers counted on Day 12. The graph illustrates the fold difference in proliferation between the GDC-treated and control (DMSO) groups on Day 12. The dashed line indicates the fold change for the control group. All experiments used control (DMSO), SB-590885 (HY-10966) at 1 μM, GDC-0879 (HY-50864) at 2 μM, and Encorafenib (HY-15605) at 0.5 μM.
GDC-0879 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]
Statistical analysis of the area of 75 individual erythroid colonies in panel on Day 14.All experiments used control (DMSO), SB-590885 (HY-10966) at 1 μM, GDC-0879 (HY-50864) at 2 μM, and Encorafenib (HY-15605) at 0.5 μM.
GDC-0879 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]
Immunoblotting of MAPK signaling cascade proteins in UCB-CD34+-derived erythroblasts cultured under normal conditions and treated on Day 9 with Encorafenib (HY-15605; 0.5 μM), GDC-0879 (HY-50864; 2 μM), or SB-590885 (HY-10966; 0.5 μM) for 30 min.
GDC-0879 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]
Levels of phosphorylated and total ERK proteins in UCB-CD34+-derived erythroblasts on Day 9, cultured under normal conditions and treated with different BRAF inhibitors (SB-590885 (HY-10966), GDC-0879 (HY-50864), Encorafenib (HY-15605)) for 30 min.
GDC-0879 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]
Flow cytometry analysis of UCB-CD34+-derived erythroid cells in the control group and GDC-0879 (2 μM)-treated group on differentiation Day 9 under normal and specified conditions (5% EPO [0.15 IU/mL EPO]; 0% SCF [0 ng/mL SCF]), using cell surface markers CD117, CD235a, and CD71, CD235a. Concentrations of other cytokines were kept unchanged as usual.
GDC-0879 purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2024 Dec 2;9(1):338. [Abstract]
Immunofluorescence staining of phosphorylated-ERK-FITC, erythroid markers CD235a-APC and CD71-PE, and DAPI of 7-day differentiated erythroid cells from UCB-CD34+ treated GDC-0879 (2 μM) for 30 min. Scale bar = 10 μm.
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077 -
Oncotarget
2017 Nov 22;8(65):109135-109150. PMID: 29312596
GDC-0879 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150. [Abstract]
MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.
Solvente y solubilidad
DMSO : 50 mg/mL (149.53 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: ≥ 2.5 mg/mL (7.48 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
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.
Protocolo
GDC-0879 in vitro IC50 estimates for pMEK inhibition are determined using A375 and Colo205 cells. In brief, A375 or Colo205 cells are incubated with a range of GDC-0879 concentrations (from 0.5 nM to 6.75 μM) for 25 min. Cells are lysed, and the lysates are subjected to centrifugation at 16,100g for 30 min, and the level of total protein is determined. Enzyme-linked immunosorbent assay kits are used to determine pMEK1 and total MEK1 protein levels in a 96-well format. Samples are analyzed in duplicate at 20 μg of protein per well. The optical densities obtained at 450 nm are converted to units per milliliter (for pMEK1) or nanograms per milliliter (for total MEK1) using a standard curve determined with recombinant pMEK1 or MEK1. The pMEK1/total MEK1 ratios are then calculated as units per nanogram. The IC50 estimates for pMEK1 inhibition are estimated by nonlinear regression using GraphPad Prism version 4.02[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Female athymic nu/nu mice (weighing 25-28 g) are administered oral doses of 15, 25, 50, 100, and 200 mg/kg GDC-0879. Blood samples (~1 mL) are collected at 0.5, 1, 2, 4, 8, and 24 h after dose via cardiac puncture (terminal collection) into tubes containing K2EDTA anticoagulant. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice. Within 30 min, blood samples are centrifuged at approximately 1000 to 1500g for 5 min at 4°C, and plasma is harvested. The plasma samples are stored at -80°C until analysis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (769 KB)
- English - EN (769 KB)
- Français - FR (769 KB)
- Deutsch - DE (769 KB)
- Norwegian - NO (769 KB)
- Español - ES (769 KB)
- Swedish - SV (769 KB)
- Italian - IT (769 KB)
- Portuguese - PT (769 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hansen JD, et al. Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. [Content Brief]
[2]. Wong H, et al. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations, phosphorylated mitogen-activated protein kinase kinase 1 inhibition, and efficacy. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9907 mL | 14.9535 mL | 29.9070 mL | 74.7675 mL |
| 5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL | 14.9535 mL | |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9907 mL | 7.4767 mL | |
| 15 mM | 0.1994 mL | 0.9969 mL | 1.9938 mL | 4.9845 mL | |
| 20 mM | 0.1495 mL | 0.7477 mL | 1.4953 mL | 3.7384 mL | |
| 25 mM | 0.1196 mL | 0.5981 mL | 1.1963 mL | 2.9907 mL | |
| 30 mM | 0.0997 mL | 0.4984 mL | 0.9969 mL | 2.4922 mL | |
| 40 mM | 0.0748 mL | 0.3738 mL | 0.7477 mL | 1.8692 mL | |
| 50 mM | 0.0598 mL | 0.2991 mL | 0.5981 mL | 1.4953 mL | |
| 60 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2461 mL | |
| 80 mM | 0.0374 mL | 0.1869 mL | 0.3738 mL | 0.9346 mL | |
| 100 mM | 0.0299 mL | 0.1495 mL | 0.2991 mL | 0.7477 mL |
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