[CAS NO. 1133432-49-1] GDC-0834

Name: GDC-0834
Brand: Arctom Scientific
SKU: AS201874

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1133432-49-1]

Fulfillment

Catalog

AS201874

Brand

Arctom Scientific

CAS

1133432-49-1

DESCRIPTION [1133432-49-1]

Overview

MDL	MFCD22665722
Molecular Weight	596.74
Molecular Formula	C33H36N6O3S
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

For research use only. We do not sell to patients.

Summary

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.

IC50 & Target

IC50: 5.9 nM (BTK) ^[1]

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.) ^[1] . 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 ^[2] .

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.) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 32 mg/mL ( 53.62 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6758 mL	8.3789 mL	16.7577 mL
5 mM	0.3352 mL	1.6758 mL	3.3515 mL
10 mM	0.1676 mL	0.8379 mL	1.6758 mL

* Please refer to the solubility information to select the appropriate solvent.

References

Synonyms

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-

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-tetrahydrobenzo[b]thiophene-2-carboxamide

GDC 0834