| Company Name: |
Haoyuan Chemexpress Co., Ltd.
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| Tel: |
021-58950125 |
| Email: |
info@chemexpress.com |
| Products Intro: |
Product Name:GDC-0834
CAS:1133432-49-1
Purity:>98% Package:2333RMB/2mg
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GDC0834 manufacturers
- GDC-0834
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- $198.00 / 2mg
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2024-10-28
- CAS:1133432-49-1
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | GDC0834 Basic information |
| Product Name: | GDC0834 | | Synonyms: | GDC 0834;GDC0834;GDC-0834;GDC-0837;CS-1263;N-[3-[6-[4-[(2R)-1,4-dimethyl-3-oxopiperazin-2-yl]anilino]-4-methyl-5-oxopyrazin-2-yl]-2-methylphenyl]-4,5,6,7-tetrahydro-1-benzothiophene-2-carboxamide;Benzo[b]thiophene-2-carboxamide, N-[3-[6-[[4-[(2R)-1,4-dimethyl-3-oxo-2-piperazinyl]phenyl]amino]-4,5-dihydro-4-methyl-5-oxo-2-pyrazinyl]-2-methylphenyl]-4,5,6,7-tetrahydro- | | CAS: | 1133432-49-1 | | MF: | C33H36N6O3S | | MW: | 596.74 | | EINECS: | | | Product Categories: | | | Mol File: | 1133432-49-1.mol |  |
| | GDC0834 Chemical Properties |
| density | 1.35±0.1 g/cm3(Predicted) | | solubility | DMSO:32.0(Max Conc. mg/mL);53.62(Max Conc. mM) | | pka | 12.46±0.70(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | GDC0834 Usage And Synthesis |
| Uses | GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively. | | in vivo | The treatment of BALB/c mice with GDC-0834 results in dose-dependent inhibition of pBTK-Tyr223. Animals dosed with 150 or 100 mg/kg GDC-0834 for 2 h show complete inhibition of pBTK-Tyr223 levels in blood, with a mean inhibition of 97 and 96%, respectively. In the rat CIA study, GDC-0834 inhibits pBTK-Tyr223 in rat blood in a dose-dependent manner. The IC50 estimate of pBTK-Tyr223 inhibition in rats is determined to be 5.6±1.6 μM with m of 0.51±0.087 (mean±S.E.)[1]. | | 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 DOI:10.1124/jpet.111.181545
[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 DOI:10.1124/dmd.114.061804 |
| | GDC0834 Preparation Products And Raw materials |
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