Fmoc-Val-Cit-PAB-OH is a cleavable useful heterobifunational linker for making Antibody-Drug-Conjugates (ADC). The Val-Cit will specifically be cleaved by catepsin B. As this enzyme is only present in the lysosome, the ADC payload will only be released in the cell. The azido group will react with DBCO, BCN or other Alkyne group through click chemistry. The PEG spacer increases aqueous solubility.
| Molecular Weight | 601.69 |
| Formula | C33H39N5O6 |
| CAS Number | 159858-22-7 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related ADC Linker Products |
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| DBCO-acid
DBCO-acid is a cleavable ADC linker used in the synthesis of ADC linker DBCO-NHS ester, and agent-linker conjugates DBCO-PEG-MMAE. |
| Boc-Gly-Gly-Phe-Gly-OH TFA
Boc-Gly-Gly-Phe-Gly-OH TFA, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC). |
| Boc-Gly-Gly-Phe-Gly-OH
Boc-Gly-Gly-Phe-Gly-OH, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC). |
| Fomc-Gly-Gly-Phe-Gly-OH
Fomc-Gly-Gly-Phe-Gly-OH can be used as an intermediate in the synthesis of ADC dual-drug-linker. |
| Mc-Gly-Gly-Phe-Gly-PAB-OH
Mc-Gly-Gly-Phe-Gly-PAB-OH (Mc-GGFG-PAB-OH) is a cleavable ADC linker used for antibody-drug conjugates (ADCs). |
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