GDC-0834 Racemate
Based on 1 publication(s) in Google Scholar
GDC-0834 Racemate is the racemic form of GDC-0834 (HY-15427). GDC-0834 is an orally active selective, potent, and reversible BTK inhibitor with an IC50 of 5.9 nM. GDC-0834 demonstrates pBTK-Tyr223 inhibition in mice and rats. GDC-0834 can be used for research of rheumatoid arthritis (RA).
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- CAS No.: 1133432-46-8
- 화학식: C33H36N6O3S
- 분자량:596.74
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
Publications Citing Use of MedChemExpress (MCE) GDC-0834 Racemate
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Biological Activity
GDC-0834 (1 h) inhibits BTK in rat splenocytes with a cellular IC50 of 6.4 nM[1].
GDC-0834 is shown to be a potent reversible inhibitor of six known aldehyde oxidase (AO) substrates with IC50 values ranging from 0.86 to 1.87 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GDC-0834 (1-100 mg/kg; p.o.; b.i.d./q.d./Q2D; 16 days) dose-dependently inhibts pBTK-Tyr223 in CIA rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice[1]
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Dosage:25, 50, 100, and 150 mg/kg
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Administration:p.o.; single dose
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Result:Showed complete inhibition of pBTK-Tyr223 levels in blood, with a mean inhibition of 97 and 96%, at 150 and 100 mg/kg, respectively.
Resulted in dose-dependent inhibition of pBTK-Tyr223.
Showed an IC50 of 1.1 μM.
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Animal Model:Female Lewis rats with arthritis[1]
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Dosage:1, 3, 10, 30, and 100 mg/kg (b.i.d.); 10, 30, 100 mg/kg (q.d.); 100 mg/kg (Q2D)
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Administration:p.o.; b.i.d./q.d./Q2D; 16 days
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Result:Inhibited pBTK-Tyr223 in rat blood in a dose-dependent manner.
Showed an IC50 of 0.51 μM.
Chemical Information
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CAS No. 1133432-46-8
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Appearance Solid
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분자량 596.74
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화학식 C33H36N6O3S
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(CCCC2)=C2S1)NC3=CC=CC(C(N=C4NC5=CC=C(C6N(C)CCN(C)C6=O)C=C5)=CN(C)C4=O)=C3C
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 100 mg/mL (167.58 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (4.19 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.
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 (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Liu L, et al. Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy. J Pharmacol Exp Ther. 2011 Jul;338(1):154-63. [Content Brief]
[2]. Sodhi JK, et al. A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834. Drug Metab Dispos. 2015 Jun;43(6):908-15 [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6758 mL | 8.3789 mL | 16.7577 mL | 41.8943 mL |
| 5 mM | 0.3352 mL | 1.6758 mL | 3.3515 mL | 8.3789 mL | |
| 10 mM | 0.1676 mL | 0.8379 mL | 1.6758 mL | 4.1894 mL | |
| 15 mM | 0.1117 mL | 0.5586 mL | 1.1172 mL | 2.7930 mL | |
| 20 mM | 0.0838 mL | 0.4189 mL | 0.8379 mL | 2.0947 mL | |
| 25 mM | 0.0670 mL | 0.3352 mL | 0.6703 mL | 1.6758 mL | |
| 30 mM | 0.0559 mL | 0.2793 mL | 0.5586 mL | 1.3965 mL | |
| 40 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0474 mL | |
| 50 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8379 mL | |
| 60 mM | 0.0279 mL | 0.1396 mL | 0.2793 mL | 0.6982 mL | |
| 80 mM | 0.0209 mL | 0.1047 mL | 0.2095 mL | 0.5237 mL | |
| 100 mM | 0.0168 mL | 0.0838 mL | 0.1676 mL | 0.4189 mL |
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