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TAO Kinase inhibitor 1

Cat. No. M14780
TAO Kinase inhibitor 1 Structure
Synonym:

CP 43

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Biological Activity

TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.

Chemical Information
Molecular Weight 384.47
CAS Number 850467-66-2
Solubility (25°C) DMSO 62.5 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] E J Neag, et al. 2021 update on thyroid-associated ophthalmopathy

[2] Yan Zhao, et al. Efficacy and Safety of SHR0302, a Highly Selective Janus Kinase 1 Inhibitor, in Patients with Moderate to Severe Atopic Dermatitis: A Phase II Randomized Clinical Trial

[3] Yu Chen, et al. A versatile polypharmacology platform promotes cytoprotection and viability of human pluripotent and differentiated cells

[4] Terry J Smith, et al. Insulin-like Growth Factor-I Receptor and Thyroid-Associated Ophthalmopathy

[5] Zhan Yao, et al. Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS

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Keywords: TAO Kinase inhibitor 1, CP 43 supplier, inhibitors, activators


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