GDC-0834
Based on 1 publication(s) in Google Scholar
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).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.05%
- CAS. Nr.: 1133432-49-1
- Formel: C33H36N6O3S
- Molecular Weight:596.74
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GDC-0834
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Biologische Aktivität
IC50: 5.9 nM (BTK)[1]
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. Nr. 1133432-49-1
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Appearance Solid
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Molecular Weight 596.74
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Formel 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([C@H]6N(C)CCN(C)C6=O)C=C5)=CN(C)C4=O)=C3C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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
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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
Lösungsmittel & Löslichkeit
DMSO : ≥ 32 mg/mL (53.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
Verweise
[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 [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 |
GDC-0834 Related Classifications
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