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TAK-020

Cat. No. M21189
TAK-020 Structure
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Biological Activity

TAK-020 is a highly selective oral covalent BTK inhibitor with a promising safety and tolerability profile for both hematologic malignancies and autoimmune diseases.

Chemical Information
Molecular Weight 351.36
Formula C18H17N5O3
CAS Number 1627603-21-7
Solubility (25°C) DMSO : 16.67 mg/mL
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] Mark Sabat, et al. J Med Chem. Correction to "Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 ( S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H-1,2,4-triazol-3-one, by Fragment-Based Drug Design"

[2] Mark Sabat, et al. J Med Chem. Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 ( S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3 H-1,2,4-triazol-3-one, by Fragment-Based Drug Design

[3] Ehsanollah Esfandiari, et al. Clin Transl Sci. A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single-Dose and Multiple-Rising-Dose Study of the BTK Inhibitor TAK-020 in Healthy Subjects

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Keywords: TAK-020 supplier, BTK, inhibitors, activators
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