GDC-0834 - 10mM in DMSO , CAS No.1133432-49-1

CAS: 1133432-49-1 Cat. No.: G656119 Formule: C₃₃H₃₆N₆O₃S Poids moléculaire: 596.7 PubChem CID: 25234918

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Vue d’ensemble

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.

IC50& Target:IC50: 5.9 nM (BTK)

Specifications

Spécifications et pureté

10mM in DMSO

Mécanismes biochimiques et physiologiques

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.

Conditions de stockage de stockage

Store at -80°C

Expédié en

Dry ice packs + Cold packs

Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.

Type d'action

INHIBITOR

Noms et identifiants

• Isomères SMILES: CC1=C(C=CC=C1NC(=O)C2=CC3=C(S2)CCCC3)C4=CN(C(=O)C(=N4)NC5=CC=C(C=C5)[C@@H]6C(=O)N(CCN6C)C)C
• CAS alternatif: 1133432-49-1
• PubChem CID: 25234918
• Termes d'entrée MeSH: GDC 0834;GDC-0834;GDC0834;N-(3-(6-(4-(1,4-dimethyl-3-oxopiperazin-2-yl)phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazin-2-yl)-2-methylphenyl)-4,5,6,7-tetrahydrobenzo(b)thiophene-2-carboxamide
• Poids moléculaire: 596.7

Cibles associées (humaines)

BTK Tclin Tyrosine-protein kinase BTK (0 Activities)

Discover Target: BTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Foire aux questions

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1133432-49-1, the molecular formula is C33H36N6O3S, and the molecular weight is 596.7 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.