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GSK2983559 free acid

Cat. No. M9426
GSK2983559 free acid Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 190  USD190 In stock
50mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

GSK2983559 free acid is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor.

Chemical Information
Molecular Weight 538.53
Formula C21H23N4O7PS2
CAS Number 1579965-12-0
Solubility (25°C) DMSO ≥ 3 mg/mL (Need ultrasonic and heat to 60°C)
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] Haile PA, et al. J Med Chem. Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

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Keywords: GSK2983559 free acid supplier, RIPK, inhibitors, activators


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