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TX2-121-1 

Cat. No. M28656
TX2-121-1  Structure
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Quality Control & Documentation
Biological Activity

TX2-121-1, a potent and selective Her3 (ErbB3) bivalent ligand, can induce degradation of Her3 with an IC50 of 49 nM. TX2-121-1 can inhibit Her3-dependent signaling.

Chemical Information
Molecular Weight 716.91
Formula C42H52N8O3
CAS Number 1603845-42-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Sang Min Lim, et al. Bioorg Med Chem Lett. Development of small molecules targeting the pseudokinase Her3

[2] Ting Xie, et al. Nat Chem Biol. Pharmacological targeting of the pseudokinase Her3

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