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TMX-4116

Cat. No. M21150
TMX-4116  Structure
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Biological Activity

TMX-4116 is a casein kinase 1α (CK1α) degradation agent. tmx-4116 shows a preference for CK1α degradation in MOLT4, Jurkat and MM.1S cells with DC50 less than 200 nM. tmx-4116 can be used in the study of multiple myeloma.

Chemical Information
Molecular Weight 389.43
Formula C17H19N5O4S
Solubility (25°C) DMSO ≥ 60 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] Mingxing Teng, et al. J Med Chem. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216

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Keywords: TMX-4116 supplier, Casein Kinase, inhibitors, activators


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