Sulfo-SMCC sodium is a commonly used hetero-bifunctional, noncleavable ADC crosslinker bearing N-hydroxysuccinimide (NHS) ester and maleimide groups to react with primary amines and sulfhydryl groups, respectively. Sulfo-SMCC is heterobifunctionalcrosslinker that contains N-hydroxysuccinimide (NHS) ester and maleimide groups that allow covalent conjugation of amine- and sulfhydryl-containing molecules. NHS esters react with primary amines at pH 7~9 to form amide bonds, while maleimides react with sulfhydryl groups at pH 6.5~7.5 to form stable thioether bonds. In aqueous solutions, NHS ester hydrolytic degradation is a competing reaction whose rate increases with pH. The maleimide group is more stable than the NHS-ester group but will slowly hydrolyze and loses its reaction specificity for sulfhydryls at pH values > 7.5. For these reasons, conjugations with these crosslinkers are usually performed at pH 7.2~7.5, with the NHS-ester (amine-targeted) reacted before or simultaneous with the maleimide (sulfhydryltargeted) reaction.
Molecular Weight | 436.37 |
Formula | C16H17N2NaO9S |
CAS Number | 92921-24-9 |
Solubility (25°C) | Water 10 mM |
Storage | 2-8°C, protect from light, dry, sealed |
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 Drug-Linker Conjugates for ADC Products |
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SC-VC-PAB-MMAE
SC-VC-PAB-MMAE is part of a drug-linker conjugate for ADC (ADC) with anticancer activity, which consists of MMAE (a tubulin inhibitor) linked to a cleavable SC-VC-PAB linker. |
DBCO-(PEG)3-VC-PAB-MMAE
DBCO-(PEG)3-vc-PAB-MMAE is an active molecule coupler (drug-linker conjugate for ADC) consisting of auristatin E attached to a DBCO-(PEG)3-vc-PAB connector. It can be used for cancer research. In addition, DBCO-(PEG)3-vc-PAB-MMAE is a click chemistry that contains a DBCO moiety and can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing an Azide moiety. |
PB038
PB038 is a drug-liker containing a PEG unit and a cleavable linker attached to Exatecan. |
Val-Ala-PAB-MMAE
Val-Ala-PAB-MMAE is a Drug-Linker Conjugate for ADC, consisting of ADC linker (Val-Ala-PAB) and MMAE. |
Val-Ala-PABC-Exatecan
Val-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (topoisomerase I inhibitor). |
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