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GDC-0834

Cat. No. M2718
GDC-0834 Structure
Size Price Availability
5mg USD 220  USD220 Out of stock
10mg USD 300  USD300 Out of stock
50mg USD 860  USD860 Out of stock
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Quality Control & Documentation
Biological Activity

GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM.

Chemical Information
Molecular Weight 596.74
Formula C33H36N6O3S
CAS Number 1133432-50-4
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jasleen K Sodhi, et al. A novel reaction mediated by human aldehyde oxidase: amide hydrolysis of GDC-0834

[2] Wendy B Young, et al. Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834

[3] Akintunde Akinleye, et al. Ibrutinib and novel BTK inhibitors in clinical development

[4] Young G Shin, et al. Validation and application of a liquid chromatography-tandem mass spectrometric method for the determination of GDC-0834 and its metabolite in human plasma using semi-automated 96-well protein precipitation

[5] Lichuan Liu, et al. Significant species difference in amide hydrolysis of GDC-0834, a novel potent and selective Bruton's tyrosine kinase inhibitor

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Keywords: GDC-0834 supplier, BTK, inhibitors, activators


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