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ITK degrader 2

Cat. No. M43518
ITK degrader 2 Structure
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Biological Activity

ITK degrader 2 is a modulator of targeted ubiquitination and a targeted protein degrading molecule.

Chemical Information
Molecular Weight 753.88
Formula C41H49F2N9O3
CAS Number 2858738-65-3
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] Tjeerd Barf et al. J Pharmacol Exp Ther. Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile

[2] Vincent Sibaud et al. Am J Clin Dermatol. Dermatological Toxicities of Bruton's Tyrosine Kinase Inhibitors

[3] Sujal Ghosh et al. J Clin Immunol. Interleukin-2-inducible T-cell kinase (ITK) deficiency - clinical and molecular aspects

[4] Baishan Jiang et al. Cell Chem Biol. ITK degradation to block T cell receptor signaling and overcome therapeutic resistance in T cell lymphomas

[5] Kristina S Lechner et al. J Mol Med (Berl). Role of the IL-2 inducible tyrosine kinase ITK and its inhibitors in disease pathogenesis

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Keywords: ITK degrader 2 supplier, Itk, inhibitors, activators

 
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