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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
46 Results for "
payload release
" in MedChemExpress (MCE) Product Catalog:
Products (46)
46 Results for "payload release" in MCE Product Catalog:
7
7 Publications Verification
Synonyms: SG3249
Research Areas:
Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity .
4
4 Cited Publications
Research Areas:
SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249) .
3
3 Cited Publications
Synonyms: DS-1062 (solution); Dato-DXd (solution)
Research Areas:
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
3
Research Areas:
Datopotamab deruxtecan (DS-1062) is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
1
1 Cited Publications
Synonyms: (Rac)-Z-Phe-Phe-FMK
Cathepsin L-IN-2 ((Rac)-Z-Phe-Phe-FMK) is a Cathepsin L (CTSL) inhibitor. Cathepsin L-IN-2 inhibits CTSL enzymatic activity, supporting the mechanism by which CTSL mediates T-DXd linker cleavage and payload release. Cathepsin L-IN-2 is used in studies on Cathepsin L-dependent ADC payload release and breast cancer-related mechanisms .
Cat. No.: HY-164702
Synonyms: Izalontamab Brengitecan
Research Areas:
BL-B01D1 (Izalontamab Brengitecan) is a bispecific antibody-drug conjugate (ADC) targeting EGFR and HER3, formed by conjugating the EGFR/HER3 bispecific antibody Izalontamab (HY-P99676) to a novel TOP-I inhibitor payload Deruxtecan 2-hydroxypropanamide (HY-153891) via a cleavable linker (Mc-Gly-Gly-Phe-Gly). BL-B01D1 binds to EGFR and HER3 on the surface of tumor cells, mediates endocytosis and releases the payload, inhibits topoisomerase I, blocks DNA replication and RNA synthesis, and disrupts DNA structure. BL-B01D1 induces cell cycle S-phase arrest, apoptosis, antibody-dependent cell-mediated cytotoxicity, and tumor cell death. BL-B01D1 can be used for cancer research .
Cat. No.: HY-P990673
Synonyms: DSTP-3086S Antibody; RG-7450 Antibody
Research Areas:
Target:
Research Areas:
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .
Cat. No.: HY-164734
CAS No.: 2610074-57-0
Synonyms: R-DXd; DS-6000
Target:
Research Areas:
Raludotatug Deruxtecan is an antibody-drug conjugate targeting CDH6, with an EC50 of 64.7 ng/mL in humans, 70.4 ng/mL in cynomolgus monkeys, and 228 ng/mL in mice. Raludotatug Deruxtecan specifically binds to CDH6 on the surface of cancer cells, triggers lysosomal internalization, and releases the DXd payload that inhibits TOP1. Raludotatug Deruxtecan induces DNA damage, Chk1 phosphorylation, caspase-3 cleavage, apoptosis, and bystander cell death. Raludotatug Deruxtecan is applicable to research related to serous ovarian cancer and renal cell carcinoma .
Cat. No.: HY-164729
Cat. No.: HY-W010162
CAS No.: 1948-31-8
Synonyms: L-Alanyl-L-alanine; Ala-Ala
Cat. No.: HY-163099
CAS No.: 2928571-43-9
Research Areas:
P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
Research Areas:
PSMA-Val-Cit-PAB-MMAE is a small-molecule conjugate targeting PSMA, with Monomethyl auristatin E (MMAE) (HY-15162) as its cytotoxic payload. PSMA-Val-Cit-PAB-MMAE binds to PSMA, thereby being delivered into PSMA-expressing prostate cancer cells. Subsequently, the Val-Cit linker is cleaved under the mediation of cathepsin B, releasing active MMAE. PSMA-Val-Cit-PAB-MMAE inhibits CYP3A4 activity (IC50 = 11.2 μM), induces intracellular ROS production and oxidative stress, disrupts the cytoskeleton through microtubule destabilization, and induces prostate cancer cell death. PSMA-Val-Cit-PAB-MMAE can be used in research related to prostate cancer .
Cat. No.: HY-42709
CAS No.: 24787-89-1
Synonyms: Carbobenzoxy-L-valyl-L-alanine
Target:
Research Areas:
Cat. No.: HY-159783
CAS No.: 3028213-52-4
Research Areas:
Mal-Exatecan is a maleimide (Mal)-modified Exatecan (HY-13631) and is a DNA topoisomerase I (topoisomerase I) inhibitor. Mal-Exatecan serves as a cytotoxic payload for antibody-drug conjugates (ADCs), conjugating to antibody cysteine residues via the maleimide group and releasing Exatecan within tumor cells to exert cytotoxic effects. Mal-Exatecan can be used for ADC construction and cancer-related research .
Cat. No.: HY-164429
CAS No.: 2418533-90-9
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
Cat. No.: HY-169323
CAS No.: 2921735-87-5
Synonyms: Mal-Exo-EEVC-MMAE
Target:
Research Areas:
APL-1091 (Mal-Exo-EEVC-MMAE) is an ADC payload-linker conjugate (Drug-Linker Conjugates for ADC). APL-1091 is formed by the conjugation of the Mal-Exo-EEVC (HY-169353) linker and MMAE (HY-15162), a microtubule inhibitor. APL-1091 resists aggregation at high drug-to-antibody ratio (DAR), exhibits excellent plasma stability, and reduces premature payload release. When conjugated with Trastuzumab (HY-P9907), APL-1091 displays anti-tumor activity in gastric cancer xenograft models. APL-1091 can be used for ADC synthesis and gastric cancer-related research .
Cat. No.: HY-173703
CAS No.: 3025108-11-3
Research Areas:
β-Glu-PAB (CH2NH2)-Exatecan is a linker-payload conjugate composed of Exatecan (HY-13631) and β-Glu-PAB (CH2NH2). β-Glu-PAB (CH2NH2)-Exatecan also serves as an intermediate of Mal ((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (HY-173634). β-Glu-PAB (CH2NH2)-Exatecan is specifically cleaved by β-glucuronidase, which is highly expressed in the tumor microenvironment, to release Exatecan that exerts cytotoxic effects. β-Glu-PAB (CH2NH2)-Exatecan can be used in cancer research .
Cat. No.: HY-169324
CAS No.: 2921735-91-1
Synonyms: Mal-Exo-EEVC-Exatecan
Target:
Research Areas:
APL-1092 is an EEVC linker-payload conjugate composed of exatecan, a stabilizer that prevents premature payload release, and a cleavage substrate for cathepsin B . APL-1092 resists premature payload release mediated by human neutrophil elastase and carboxylesterase, maintains payload stability in mouse plasma, and retains cathepsin B-mediated cleavage activity in target cells . APL-1092 exhibits dose-dependent tumor growth inhibition in xenograft mice . APL-1092 can be used in gastric cancer-related research .
Cat. No.: HY-128952G
CAS No.: 1595275-62-9
Synonyms: SG3249 (GMP)
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
