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Boc-Val-Cit-PAB

Cat. No. M10413
Boc-Val-Cit-PAB Structure
Synonym:

Boc-Val-Cit-PABA

Size Price Availability
100mg USD 160  USD160 Custom Synthesis
250mg USD 280  USD280 Custom Synthesis
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Quality Control & Documentation
Biological Activity

Boc-Val-Cit-PAB is a cleavable ADC linker used in making antibody-drug conjugates (ADCs). The Val-Cit will specifically be cleaved by catepsin B. As this enzyme is only present in the lysosome the ADC payload will be release only in the cell. The Boc group can be deprotected under acidic conditions to generate a free amine group.

Chemical Information
Molecular Weight 479.57
Formula C23H37N5O6
CAS Number 870487-09-5
Solubility (25°C) DMSO
Storage 2-8°C, dry, sealed
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] Alain Beck, et al. Nat Rev Dгυg Discov. Strategies and challenges for the next generation of antibody-dгυg conjugates

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