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
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
HY-17600
AcalabrutinibBTK Inhibitor -
HY-112215
NemtabrutinibBTK Inhibitor -
HY-10997
IbrutinibBtk Inhibitor -
HY-19834
FenebrutinibBtk Inhibitor -
HY-19730
OlmutinibEGFR Tyrosine Kinase Inhibitor -
HY-101474A
ZanubrutinibBtk Inhibitor -
HY-112166
RilzabrutinibBTK Inhibitor -
HY-15771
TirabrutinibBTK Inhibitor -
HY-100342
Ibrutinib-biotinProbe -
HY-18012
Spebrutinib -
HY-112161
BranebrutinibBTK Inhibitor -
HY-101474AR
Zanubrutinib (Standard)Btk Inhibitor
Publications Citing Use of MedChemExpress (MCE) GDC-0834
More
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 5.9 nM (BTK)[1]
In Vitro
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. Further protocols information, click here.
In Vivo
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.
-
Animal Model:BALB/c mice[1]
-
Dosage:25, 50, 100, and 150 mg/kg
-
Administration:p.o.; single dose
-
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.
-
Animal Model:Female Lewis rats with arthritis[1]
-
Dosage:1, 3, 10, 30, and 100 mg/kg (b.i.d.); 10, 30, 100 mg/kg (q.d.); 100 mg/kg (Q2D)
-
Administration:p.o.; b.i.d./q.d./Q2D; 16 days
-
Result:Inhibited pBTK-Tyr223 in rat blood in a dose-dependent manner.
Showed an IC50 of 0.51 μM.
Chemical Information
-
CAS. Nr. 1133432-49-1
-
Appearance Solid
-
Molecular Weight 596.74
-
Formel C33H36N6O3S
-
Color Light yellow to yellow
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
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
In Vitro:
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)
Protokoll
-
Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
-
Data Sheet (275 KB)
-
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)
-
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
HY-15427 Related Classifications
Powered by Bioz