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

CAS: 1133432-49-1 Cat. No.: G656119 분자식: C₃₃H₃₆N₆O₃S 분자량: 596.7 PubChem CID: 25234918

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

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

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

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.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

이름과 식별자

• 이성체 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
• 대체 CAS: 1133432-49-1
• PubChem CID: 25234918
• MeSH 용어: 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
• 분자량: 596.7

관련 대상(인간)

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)

자주 묻는 질문

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.