GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC 50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC 50 of 1.1 and 5.6 μM in mouse and rat, respectively. In Vitro GDC-0834 suppresses BTK kinase activity with an IC 50 value of 5.9±1.1 nM with Hill slope value of −0.84±0.07 (mean±S.E.). GDC-0834 is shown to be a potent reversible inhibitor of six known aldehyde oxidase (AO) substrates with IC 50 values ranging from 0.86 to 1.87 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 IC 50 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.) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 5.9 nM (BTK)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
GDC-0834
CAS number：1133432-49-1 molecular formula：C33H36N6O3S
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 1133432-49-1 | DTXSID001025916 | CDOOFZZILLRUQH-GDLZYMKVSA-N | BDBM50388183 | 2VL | FM7JG3L4SR | 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 | UNI | ||
| CAS number | 1133432-49-1 | molecular formula | C33H36N6O3S |
| molecular weight | 596.7 g/mol | Exact mass | ≥98% |
| PSA | 126.000 Ų | logp | 4.300 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
