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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.05%
- CAS 番号: 1133432-49-1
- 分子式: C33H36N6O3S
- 分子量:596.74
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保管条件: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]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 GDC-0834
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生物活性
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.
化学情報
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CAS 番号 1133432-49-1
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性状 Solid
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分子量 596.74
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-15427 関連分類
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