Antibody-drug Conjugates (ADC)

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  1. Fmoc-Val-Cit-PAB-PNP is a cleavable peptide linker, is a linker for antibody-drug-conjugation (ADC).
  2. Fmoc-Val-Cit-PAB is a cleavable linker for antibody-drug-conjugation (ADC).
  3. 2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocycle DOTA derivative for tumor pretargeting.
  4. antibody-drug conjugate Linker

    Ozogamicin is an antibody-drug conjugate Linker.
  5. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
  6. Monomethyl auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin, and also shows inhibition of antibody-drug conjugates (ADCs) activity.
  7. cleavable ADC linker

    Mc-Val-Cit-PAB-Cl is a cleavable ADC linker. Mc-Val-Cit-PAB-Cl can be used to conjugate MMAE and antibody to form antibody-MC-vc-MMAE .
  8. Daunorubicinol is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (DNA Topoisomerase II inhibitor), linked via the ADC linker.
  9. Vc-seco-DUBA is a drug-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco.
  10. MC-VC-PABC-Aur0101 is a drug-linker conjugate for ADC with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the ADC linker MC-VC-PABC.
  11. Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent. It is part of some experimental anti-cancer antibody-drug conjugates such as vorsetuzumab mafodotin and SGN-CD19A.
  12. VcMMAE is an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
  13. Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
  14. Tubulin inhibitor

    Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulin inhibitor (MMAD), Vc-MMAD is an antibody drug conjugate.
  15. ADC peptide linker

    Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC peptide linker.
  16. Biotin PEG Linker

    Biotin-PEG3-amineis PEG derivative containing a biotin group and a terminal primary amine group.
  17. PSMA-617, also know as vipivotide tetraxetan. It is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer.
  18. cleavable ADC linker

    CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours).
  19. DNA Topoisomerase I inhibitor

    CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types.
  20. L2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.
  21. cleavable linker

    EC089 is a cleavable linker used in conjugates of tubulysins and folates, and extracted from patent WO2011069116A1.
  22. EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC).
  23. 6-O-2-Propyn-1-yl-D-galactose is a nonclaevable glycolinker for the functionalization of cytotoxic drugs and applications in antibody-drug conjugation.
  24. Fmoc-PEA (Example 1-2) is a used as a cleavable linker for antibody-drug conjugates (ADC).
  25. SPP is a cleavable disulfide linker, can be used to form cytotoxic compound- linker conjugate.
  26. heterobifunctional crosslinker

    AMAS is a nonclaevable heterobifunctional crosslinker with NHS ester and maleimide groups that allows covalent conjugation of amine- and sulfhydryl-containing molecules.
  27. Duocarmycin is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity. Duocarmycin is a DNA minor groove binding alkylating agent and explored as drug?Cantibody conjugates (ADCs) .
  28. MC-Val-Cit-PAB-tubulysin5a is a drug-linker conjugate for ADC with potent antitumor activity by using tubulysin5a (a tubulin inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  29. MC-Val-Cit-PAB-rifabutin is a drug-linker conjugate for ADC with potent antitumor activity by using rifabutin (an DNA-dependent RNA polymerase inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  30. MC-Val-Cit-PAB-Indibulin is a drug-linker conjugate for ADC with potent antitumor activity by using Indibulin (an orally applicable inhibitor of tubulin assembly), linked via the ADC linker MC-Val-Cit-PAB.
  31. protein synthesis inhibitor

    MC-Val-Cit-PAB-clindamycin is a drug-linker conjugate for ADC with potent antitumor activity by using clindamycin (a protein synthesis inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  32. MC-Val-Cit-PAB-Retapamulin is a drug-linker conjugate for ADC with potent antitumor activity by using Retapamulin (a ribosome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  33. MC-Val-Cit-PAB-dimethylDNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using dimethylDNA31, linked via the ADC linker MC-Val-Cit-PAB.
  34. MC-Val-Cit-PAB-duocarmycin is a drug-linker conjugate for ADC with potent antitumor activity by using duocarmycin (a DNA minor groove binding alkylating agent), linked via the ADC linker MC-Val-Cit-PAB.
  35. MC-Val-Cit-PAB-carfilzomib is a drug-linker conjugate for ADC with potent antitumor activity by using carfilzomib (an irreversible proteasome inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  36. MC-Val-Cit-PAB-vinblastine is a drug-linker conjugate for ADC with potent antitumor activity by using vinblastine (an microtubule protein inhibitor), linked via the ADC linker MC-Val-Cit-PAB.
  37. MC-Val-Cit-PAB-Auristatin E is a drug-linker conjugate for ADC with potent antitumor activity by using Auristatin E (a cytotoxic tubulin modifier), linked via the ADC linker MC-Val-Cit-PAB.
  38. MC-VC-PABC-DNA31 is a drug-linker conjugate for ADC with potent antitumor activity by using DNA31 (a potent RNA polymerase inhibitor), linked via the ADC linker MC-VC-PABC.
  39. Nitro-PDS-Tubulysin M is a drug-linker conjugate for ADC with potent antitumor activity by using Tubulysin M (a tubulin polymerization inhibitor), linked via the ADC linker Nitro-PDS.
  40. tubulin polymerization inhibitor

    MC-Sq-Cit-PAB-Dolastatin10 is a drug-linker conjugate for ADC with potent antitumor activity by using Dolastatin10 (a tubulin polymerization inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
  41. PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
  42. MC-Sq-Cit-PAB-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using Gefitinib (an EGFR tyrosine kinase inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
  43. DNA alkylating agent

    (+)-CBI-CDPI2 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI2 is an antibody drug conjugates (ADCs) toxin.
  44. DNA alkylating agent

    (+)-CBI-CDPI1 is an enhanced functional analog of CC-1065. (+)-CBI-CDPI1 is a DNA alkylating agent. (+)-CBI-CDPI1 is an antibody drug conjugates (ADCs) toxin.
  45. DNA alkylating agent

    Duocarmycin GA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-drug resistant cell lines.
  46. Microtubule inhibitor

    VCP-Eribulin consists the ADCs linker (VCP) and Eribulin. Eribulin is a mechanistically unique microtubule inhibitor for cancer. VCP-Eribulin is an Eribulin-based drug for antibody conjugates.
  47. Microtubule inhibitor

    Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin. Eribulin is a mechanistically unique microtubule inhibitor for cancer. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for antibody conjugates.
  48. MC-GGFG-DX8951 is a drug-linker conjugate for ADC with antitumor activity by using DX8951 (a DNA topoisomerase I inhibitor), linked via the protease cleavable MC-GGFG linker.
  49. DBCO-NHS ester 2 is a cleavable linker that is used for making antibody-drug conjugate (ADC). DBCO-NHS ester 2 is a derivative of Dibenzylcyclooctyne (DBCO) used in copper-free click chemistry.
  50. DNA topoisomerase I inhibitor

    CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor.

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