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Code Name Synonym
CH-053 trans-4-Azidocyclohexanecarboxylic acid N3-1,4-trans-CHC-OH
CAS 1931895-14-5 /upload/more_svg/small/small_CH-053.svg
Formula C7H11N3O2
MW 169.2
Purity >99%
Storage +2 ... +8 °C
Code Name Synonym
CH-055 Boc,Me-AMCHC Boc-N-methyl-tranexamic acid // trans-4-(Boc-methylaminomethyl)cyclohexane carboxylic acid
CAS 165947-29-5 /upload/more_svg/small/small/small_CH-055.svg
Formula C14H25NO4
MW 271.4
Purity >99%
Storage +2 ... +8 °C
Note Boc,Me-AMCHC is used as a protected N-methyl-Tranexamic acid building block that can be used in peptide synthesis. Bioorg. Med. Chem. Lett. (2017), 27(20), 4755-4759. DOI:10.1016/j.bmcl.2017.08.052; PCT Int. Appl. (2018), WO 2018183654 A1.
Code Name Synonym
CH-038 Fmoc-AMCHC Fmoc-Tranexamic acid // trans-4-(Fmoc-aminomethyl)cyclohexane carboxylic acid // N-Fmoc-Tranexamic acid
CAS 167690-53-1 /upload/small/small_ch-038.svg
Formula C23H25NO4
MW 379.5
Purity >99%
Storage +2 ... +8 °C
Note Fmoc-AMCHC is used as a linker in solid-phase peptide synthesis to construct various biologically active conjugates. This fragment is present in many Antibody Drug Conjugates (Kadcyla®, IMMU-132). J. Med. Chem. (2016), 59(5), 1761-1775.  DOI:10.1021/acs.jmedchem.5b01210; Behrens et al PCT Int. Appl. (2011), WO 2011089255 A1; Zhu et al PCT Int. Appl. (2019), WO 2019011166 A1.
Code Name Synonym
CH-056 Fmoc,Me-AMCHC Fmoc-N-methyl-tranexamic acid // trans-4-(Fmoc-methylaminomethyl)cyclohexane carboxylic acid
CAS 173690-50-1 /upload/more_svg/small/small/small_CH-056.svg
Formula C24H27NO4
MW 393.5
Purity >99%
Storage +2 ... +8 °C
Note Fmoc,Me-AMCHC is used as a protected N-methyl-Tranexamic acid building block that can be used in peptide synthesis. Tetrahedron Lett. (1996), 37(2), 263-6. DOI:10.1016/0040-4039(95)02145-0.
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 /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
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.

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