GDC-0134
Based on 1 Customer Validation
GDC-0134 (RG6000) is a modulator targeting dual leucine zipper kinase (DLK) that can cross the blood-brain barrier. By inhibiting the kinase activity of DLK, GDC-0134 blocks the activation of the downstream JNK signaling pathway, suppresses DLK-dependent retrograde signal transduction of axon-to-soma degeneration, and exerts neuroprotective activity. GDC-0134 reduces TDP-43 protein aggregation and decreases the degree of neuromuscular junction denervation in motor neurons. GDC-0134 can be used in the research of amyotrophic lateral sclerosis (ALS), Alzheimer's disease and other DLK-related neurodegenerative diseases.
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- Purity: 99.18%
- CAS No.: 1637394-01-4
- 화학식: C19H20F4N6O2
- 분자량:440.39
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
GNE-3511 (HY-12947), a structurally homologous DLK kinase inhibitor of GDC-0134, disrupts neurofilament 200 (NF200) and βIII-tubulin, leading to axonal cytoskeleton disorganization, in in vitro cultured dorsal root ganglion (DRG) neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GDC-0134 inhibits the activation of the JNK pathway downstream of DLK in the SOD1G93A mouse ALS model, and reduces the degree of denervation at neuromuscular junctions in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1637394-01-4
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Appearance Solid
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분자량 440.39
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화학식 C19H20F4N6O2
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Color White to off-white
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SMILES
NC1=C(C=C(C=N1)C2=NC(N3CC(F)(CC3)F)=NC(N4C[C@H]5OC[C@@H]4C5)=C2)OC(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (227.07 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: ≥ 2.5 mg/mL (5.68 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.68 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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 | 2.2707 mL | 11.3536 mL | 22.7071 mL | 56.7679 mL |
| 5 mM | 0.4541 mL | 2.2707 mL | 4.5414 mL | 11.3536 mL | |
| 10 mM | 0.2271 mL | 1.1354 mL | 2.2707 mL | 5.6768 mL | |
| 15 mM | 0.1514 mL | 0.7569 mL | 1.5138 mL | 3.7845 mL | |
| 20 mM | 0.1135 mL | 0.5677 mL | 1.1354 mL | 2.8384 mL | |
| 25 mM | 0.0908 mL | 0.4541 mL | 0.9083 mL | 2.2707 mL | |
| 30 mM | 0.0757 mL | 0.3785 mL | 0.7569 mL | 1.8923 mL | |
| 40 mM | 0.0568 mL | 0.2838 mL | 0.5677 mL | 1.4192 mL | |
| 50 mM | 0.0454 mL | 0.2271 mL | 0.4541 mL | 1.1354 mL | |
| 60 mM | 0.0378 mL | 0.1892 mL | 0.3785 mL | 0.9461 mL | |
| 80 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7096 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2271 mL | 0.5677 mL |
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