- Signaling Pathways
- Antibody-Drug Conjugate/ADC Related
- Drug-Linker Conjugates for ADC
Drug-Linker Conjugates for ADC
Drug-Linker Conjugates for Antibody Drug Conjugates (ADCs) comprise of an active cytotoxic drug and an appropriate linker. After linked to a monoclonal antibody, those conjugates can be used for making ADCs, which are targeted agents for cancer cells with high selectivity and cytotoxicity.
The drug units in drug-linker conjugates are cytotoxic agents (i.e. ADC cytotoxins or payloads) with antitumor activity and can be classified in DNA damaging agents and tubulin inhibitors. The most commonly used DNA damaging agents in ADCs are Duocarmycins, Pyrrolobenzodiazepines, Camptothecins and Daunorubicins/Doxorubicins, while the popular tubulin inhibitors are Auristatins and Maytansinoids. Besides, there are also many traditional cytotoxic agents can be used in ADCs.
ADC linkers currently undergoing clinical evaluation are mostly classified into two categories: cleavable and noncleavable. Cleavable linkers rely on processes inside the cell to liberate the toxin, and noncleavable linkers require proteolytic degradation of the antibody portion of the ADC for release of the cytotoxic molecule.
Drug-Linker Conjugates for ADC Isoform Specific Products
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Drug-Linker Conjugates for ADC
(327)
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Auristatin
(45)
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Camptothecins
(33)
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Daunorubicins/
Doxorubicins (5)View all products
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Duocarmycins
(8)
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Maytansinoids
(19)
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Pyrrolobenzodiazepines
(5)
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Traditional Cytotoxic Agents
(31)
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Dual payloads
(5)
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Drug-Linker Conjugates for ADC Related Products (500)
Related Products (500)
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Drug-Linker Conjugates for ADC Isoform Comparison
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DBCO-PEG3-VC-Exatecan
0 ImagesDBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). -
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N3-PEG3-vc-PAB-MMAE
0 ImagesN3-PEG3-vc-PAB-MMAE is a synthesized agent-linker conjugate for ADC that incorporates the MMAE (a tubulin inhibitor ) and 3-unit PEG linker. N3-PEG3-vc-PAB-MMAE shows potent antitumor activity. N3-PEG3-vc-PAB-MMAE is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups. -
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Mal-PEG2-VCP-Eribulin
0 ImagesMal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin (HY-13442). Eribulin is a mechanistically unique microtubule inhibitor and Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules. Mal-PEG2-VCP-Eribulin is an Eribulin-based agent for antibody conjugates. -
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Vc-seco-DUBA
0 ImagesSynonyms: DuocarmazineVc-seco-DUBA (Duocarmazine) is a agent-linker conjugate for ADC with potent antitumor activity by using DUBA (DNA alkylating agent), linked via the ADC linker Vc-seco. -
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TCO-PEG4-VC-PAB-MMAE
0 ImagesTCO-PEG4-VC-PAB-MMAE is a agent-linker conjugate for ADC. TCO-PEG4-VC-PAB-MMAE contains a cleavable ADC linker (TCO-PEG4-VC-PA) and a potent tubulin inhibitor MMAE (HY-15162). TCO-PEG4-VC-PAB-MMAE is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups. -
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Mal-(CH2)5-Val-Cit-PAB-Eribulin
0 ImagesMal-(CH2)5-Val-Cit-PAB-Eribulin is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-microtubule agent, Eribulin, linked via linker Mal-(CH2)5-Val-Cit-PAB. -
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Lys-SMCC-DM1
0 ImagesSynonyms: Lys-Nε-MCC-DM1Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is a agent-linker conjugates for ADC that can inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is a HER2-targeting ADC with a tubulin polymerization inhibitor DM1. Lys-SMCC-DM1 can be used in the research of breast cancer. -
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Mal-Bal-Ph(β-D-Glucose)-7-MAD-MDCPT
0 ImagesMal-Bal-Ph(β-D-Glucose)-7-MAD-MDCPT (example 70) is an ADC drug-linker conjugate composed of the Camptothecin analog 7-MAD-MDCPT (HY-132162), and a Mal-Bal-Ph(β-D-Glucose) linker. DBCO-PEG2-C2-acid can be used to synthesize antibody-drug conjugates (ADCs). -
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SC-VC-PAB-MMAE
0 ImagesSynonyms: NHS-VC-PAB-MMAESC-VC-PAB-MMAE (NHS-VC-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker SC-VC-PAB. -
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Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan
0 ImagesMal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a bioactive drug-linker conjugate for ADC (Drug-Linker Conjugates for ADC). Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is applicable to ADC synthesis and cancer research. Exatecan acts as a DNA Topoisomerase I inhibitor. -
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Amino-PEG4-Val-Cit-PAB-MMAE
0 ImagesAmino-PEG4-Val-Cit-PAB-MMAE is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). -
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DBCO-(PEG2-VC-PAB-MMAE)2
0 ImagesDBCO-(PEG2-VC-PAB-MMAE)2 is made by MMAE conjugated to the cleavable DBCO-(PEG2-VC-PAB)2 linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody agent conjugate. DBCO-(PEG2-VC-PAB-MMAE)2 is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups. -
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MC-VC-PABC-Aur0101
0 ImagesMC-VC-PABC-Aur0101 is a agent-linker conjugate for ADC with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the ADC linker MC-VC-PABC. -
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Val-Ala-PABC-Exatecan
0 ImagesVal-Ala-PABC-Exatecan is a Drug-Linker Conjugates for ADC, consiting of a cleavable Tesirine linker (Val-Ala-PABC) and Exatecan (HY-13631) (topoisomerase I inhibitor). Val-Ala-PABC-Exatecan can be used for ADC molecues synthesis, such as Mal-PEGn-amide-va-Exatecan. -
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MC-GGFG-AM-(10Me-11F-Camptothecin)
0 ImagesMC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells. -
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PEG4-aminooxy-MMAF
0 ImagesSynonyms: Amberstatin; AS269PEG4-aminooxy-MMAF is a agent-linker conjugate for ADC with potent antitumor activity by using the potent antitubulin agent MMAF, linked via the noncleavable PEG4. -
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MC-EVCit-PAB-MMAE
0 ImagesMC-EVCit-PAB-MMAE (Linker-Payload 11) is a drug-linker conjugates for ADC. MC-EVCit-PAB-MMAE contains the ADCs linker (MC-EVCit-PAB) and a potent tubulin polymerization inhibitor MMAE (HY-15162). -
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MC-SN38
0 ImagesMC-SN38 is a agent-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody agent conjugate (ADC). SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks. -
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Bi-Mc-VC-PAB-MMAE
0 ImagesBi-Mc-VC-PAB-MMAE consists ADCs linker (Bi-Mc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE, HY-15162). Bi-Mc-VC-PAB-MMAE is a drug-linker conjugate for ADC. -
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