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Code Name Synonym
ET-075 Mal-AMCHC 4-(maleimidomethyl)cyclohexane-1-carboxylic acid // trans-4-[(2,5-Dihydro-2,5-dioxo-1H-pyrrol-1-yl)methyl]cyclohexanecarboxylic acid
CAS 69907-67-1 /upload/more_svg/small/small_ET-075.svg
Formula C12H15NO4
MW 237.3
Purity >99%
Storage +2 ... +8 °C
Note Mal-AMCHC is used as a linker in various applications. It is employed as an antibody-drug linker in approved cancer medication Kadcyla by Genentech/Roche and used as a linker in PCA-062 by Novartis, currently in clinical trials. It is also used in IMMU-132 by Immunomedics, currently in clinical trials.
Code Name Synonym
ET-156 Mal(Br2)-AMCHC 3,4-dibromo-maleimido-AMCHC // 3,4-dibromo-maleimido tranexamic acid // trans‐4‐[(3,4‐dibromo‐2,5‐dioxo‐2,5‐dihydro‐1H‐ pyrrol‐1‐yl)methyl]cyclohexane‐1‐carboxylic acid
CAS n/a /upload/small/small_et-156.svg
Formula C12H13Br2NO4
MW 395
Purity >98%
Storage +2 ... +8 °C
Note Mal(Br2)-AMCHC is used as a bio-conjugation reagent for antibody-drug-conjugate synthesis. The di-bromo maleimide is a novel conjugation tool that addresses the retro-Michael instability of simple thiosuccinimide linkage. Chudasama V. et al. Drug Discovery Today: Tech. (2018), 30, 27-34. DOI:10.1016/j.ddtec.2018.07.002;  Bioconjugate Chem. (2011), 22(2), 132-136. DOI:10.1021/bc1004685; J. Am. Chem. Soc. (2012), 134(3), 1847-1852. DOI:10.1021/ja210335f; Bioconjugate Chem. (2018), 29(2), 486-492. DOI:10.1021/acs.bioconjchem.7b00795.
Code Name Synonym
ET-129 Mal(3-Me)-AMCHC 4-[(metylmaleimido)methyl]cyclohexane-1-carboxylic acid // (1r,4r)-4-[(3-methyl-2,5-dioxopyrrol-1- yl)methyl]cyclohexane-1-carboxylic acid
CAS 71738-82-4 /upload/more_svg/small/small_et-129.svg
Formula C13H17NO4
MW 251.3
Purity >99%
Storage +2 ... +8 °C
Note

Introduction of methyl group at maleimide core improves stability of maleimide-thiol conjugates.

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Code Name Synonym
ET-066 Mal-AMCHC-OSu SMCC // trans-N-Succinimidyl 4-(maleimidomethyl)cyclohexane-1-carboxylate // N-Succinimidyl 4-(Maleimidomethyl)cyclohexane-1-carboxylate
CAS 71875-81-5, 64987-85-5 /upload/more_svg/small/small_ET-066.svg
Formula C16H18N2O6
MW 334.3
Purity >99%
Storage +2 ... +8 °C
Note Used as a linker for ADC construction. ACS Omega, 2019, 8834; DOI: 10.1021/acsomega.9b00430.
Code Name Synonym
ET-174 Mal-AMCHC-N-Propargylamide MCC-Yne // trans‐4‐[(2,5‐dioxo‐2,5‐dihydro‐1H‐pyrrol‐1‐ yl)methyl]‐N‐(prop‐2‐yn‐1‐yl)cyclohexane‐1‐carboxamide // SMCC Propargyl amide // Maleimido-AMCHC-Propargylamide // Mal-AMCHC-N-Propynyl
CAS 2027476-42-0, 1036847-90-1 (cis,trans) /upload/small/small_et-174.svg
Formula C15H18N2O3
MW 274.3
Purity >98%
Storage +2 ... +8 °C
Note Used as a bio-conjugation reagent for antibody-drug-conjugate synthesis using Click-Chemistry. WO2019154120A1; US20160303253A1; US20170360770A1; Govindan, S. V. et. al. J. Med. Chem. 2008, 6916, DOI:10.1021/jm800719t.
Code Name Synonym
AA-150 H-Abu(3-N3).HCl (2S,3R) (2S,3R)-2-amino-3-azidobutanoic acid hydrochloride
CAS /upload/more_svg/small/small_AA-150.svg
Formula C4H9ClN4O2
MW 180.6
Purity >98%
Storage +2 ... +8 °C
Note H-Abu(3-N3) is incorporated into peptides and proteins that can be further selectively modified using Staudinger ligation or Click-chemistry.
Code Name Synonym
AA-149 H-Abu(3-N3).HCl (2S,3S) (2S,3S)-2-amino-3-azidobutanoic acid hydrochloride
CAS /upload/more_svg/small/small_AA-149.svg
Formula C4H9ClN4O2
MW 180.6
Purity >98%
Storage +2 ... +8 °C
Note H-Abu(3-N3) is incorporated into peptides and proteins that can be further selectively modified using Staudinger ligation or Click-chemistry.
Code Name Synonym
FM-261 Fmoc-Abu(3-NH2).HCl(2S,3S) 2-(Fmoc-amino)-3-amino butanoic acid // Fmoc-allo-azaThr // Fmoc-L-allo-azaThr-OH
CAS 244052-24-2, 788808-40-2 (net) /upload/small/small_fm-261.svg
Formula C19H21ClN2O4
MW 376.8
Purity >98%
Storage +2 ... +8 °C
Code Name Synonym
FM-181 Fmoc-Abu(3-N3) (2R,3R) (2R,3R)-(Fmoc-amino)-3-azidobutanoic acid
CAS 1229394-75-5 /upload/more_svg/small/small_FM-181.svg
Formula C19H18N4O4
MW 366.4
Purity >98%
Storage +2 ... +8 °C
Note Protected building-block for the synthesis of 2,3-diaminobutanoic acid containing peptides and also for "click" reactions. Eur. J. Org. Chem. (2010), (13), 2536-2543. DOI:10.1002/ejoc.200901345.
Code Name Synonym
FM-208 Fmoc-Abu(3-N3) (2R,3S) (2R,3S)-(Fmoc-amino)-3-azidobutanoic acid
CAS 1932349-21-7 /upload/more_svg/small/small_fm-208.svg
Formula C19H18N4O4
MW 366.4
Purity >98%
Storage +2 ... +8 °C

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