41 Results for "

antitumor payload

" in MedChemExpress (MCE) Product Catalog:
Products (41)

41 Results for "antitumor payload" in MCE Product Catalog:

7
7 Publications Verification
Cat. No.: HY-128952
CAS No.: 1595275-62-9
Purity:  98.10%
Synonyms: SG3249
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 .
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3
3 Cited Publications
Cat. No.: HY-164992
Synonyms: MRG002; Trastuzumab MMAE
Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a Kd of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma .
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3
3 Cited Publications
Cat. No.: HY-12460
CAS No.: 1626359-62-3
Purity:  98.14%
Research Areas:  

Cancer

SPDB-DM4 is a agent-linker conjugate for ADC by using the maytansinebased payload (DM4, a tubulin inhibitor) via a SPDB linker, exhibiting potent anti-tumor activity.
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Cat. No.: HY-P990673
Synonyms: DSTP-3086S Antibody; RG-7450 Antibody

Research Areas:  

Cancer

Vandortuzumab (DSTP-3086S Antibody; RG-7450 Antibody) is a humanized anti-STEAP1 IgG1 antibody and antimitotic agent that can be conjugated with MMAE (HY-15162) to form the antibody-drug conjugate (ADC) Vandortuzumab vedotin. Vandortuzumab vedotin specifically binds to STEAP1 and drives internalization of the complex, releasing the MMAE (HY-15162) payload intracellularly. After binding to tubulin, MMAE inhibits cell division and induces cell death. Vandortuzumab exhibits antitumor activity in preclinical xenograft models of prostate cancer and can be used for research related to metastatic castration-resistant prostate cancer (mCRPC) .
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Cat. No.: HY-150233
CAS No.: 1160590-05-5
Purity:  99.91%
Target:  

Microtubule/Tubulin

Research Areas:  

Cancer

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) .
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Cat. No.: HY-177434
CAS No.: 2873366-83-5
Synonyms: Precem-TcT; M 9140
Precemtabart tocentecan (Precem-TcT; M 9140) is an anti-CEACAM5 (carcinoembryonic antigen-related cell adhesion molecule 5) antibody-drug conjugate (ADC). Precemtabart tocentecan consists of a tumor-specific anti-CEACAM5 monoclonal antibody Precemtabart (HY-P990940), a highly hydrophilic and stable cleavable β-glucuronide linker, and a topoisomerase 1 inhibitor payload Exatecan (HY-13631), and the drug-linker conjugate for ADC is Mal-Gly-PAB-Exatecan-D-glucuronic acid (HY-153179). Precemtabart tocentecan inhibits the growth of CEACAM5-positive cancer cells. Precemtabart tocentecan exhibits significant antitumor activity in CEACAM5-expressing xenograft models. Precemtabart tocentecan can be used for the study of CEACAM5-expressing advanced solid tumors, especially mCRC .
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Cat. No.: HY-171124
Synonyms: AZD9592
Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research .
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Cat. No.: HY-177442
Synonyms: DS-3939
DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers .
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Cat. No.: HY-164919
CAS No.: 2847102-44-5
Synonyms: XMT-2056
Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate (ADC) targeting HER2, linked to a payload composed of XMT-1519 conjugate-1 (HY-148067) and STING agonist-20 (HY-148068). Calotatug ginistinag activates the STING signaling pathway in tumor cells and tumor-resident immune cells, induces the production of type I interferons and cytokines (CXCL10, IFN-β, IL-6, TNF-α, triggers innate anti-tumor immune responses, and exerts a bystander effect. Calotatug ginistinag exhibits efficacy against HER2-expressing cancer cells in co-culture with PBMCs. Calotatug ginistinag induces tumor regression and reduces systemic inflammation in various tumor models. Combination treatment with Calotatug ginistinag, Trastuzumab (HY-P9907) and T-DXd (HY-138298) yields benefits. Calotatug ginistinag can be used in studies related to HER2-expressing solid tumors such as breast cancer, gastric cancer and ovarian cancer .
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Cat. No.: HY-79490
CAS No.: 2922852-48-8
Research Areas:  

Cancer

Ac-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells .
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Cat. No.: HY-148127
CAS No.: 1802499-21-3
Purity:  99.29%
Research Areas:  

Cancer

TAM558 is a payload molecule used for the synthesis of OMTX705. OMTX705 is a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470 (HY-148128), with antitumor activity .
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Cat. No.: HY-144880
CAS No.: 1977557-86-0
Purity:  99.52%
Synonyms: 3-Aminophenyl Hemiasterlin
Research Areas:  

Cancer

SC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules .
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Cat. No.: HY-178836
CAS No.: 3077488-78-6
Research Areas:  

Cancer

Z56-L23 is a conjugate of RAS-targeting ADC cytotoxic payload-linker with anti-tumor activity. Z56-L23 can be conjugated with HER3 antibody, EGFR antibody or EGFRxHER3 bispecific antibody to form intact antibody-drug conjugates (ADCs). ADC molecules related to Z56-L23 effectively inhibit the proliferation of tumor cells and also significantly suppress tumor growth in xenograft mouse models. Z56-L23 can be used in the research of pancreatic cancer .
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Cat. No.: HY-114256
CAS No.: 1610413-96-1
Target:  

PSMA

Research Areas:  

Cancer

EC1169 is a cytotoxic maytansinoid conjugate that specifically binds to prostate-specific membrane antigen (PSMA). EC1169 precisely delivers the maytansinoid B hydrazide payload to PSMA-positive cells to exert antitumor activity. EC1169 only inhibits the growth of PSMA-positive cells but has no effect on PSMA-negative cells, and enables complete recovery in mice bearing PSMA-positive tumors. EC1169 exhibits safety with no body weight loss or major organ damage induced. EC1169 is used in studies of prostate cancer and other PSMA-expressing malignancies .
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Cat. No.: HY-177578
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
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Cat. No.: HY-148128
CAS No.: 1802498-63-0
Purity:  98.53%
Research Areas:  

Cancer

TAM470 is a novel cytolysin, inhibiting tubulin polymerization and microtubule depolymerization. TAM470 can be used in the synthesis of OMTX705 as payload molecule, OMTX705 is a novel FAP-targeting antibody-drug conjugates (ADCs) with antitumor activity .
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Cat. No.: HY-177585
CAS No.: 3025473-38-2
Synonyms: BLD1102
Research Areas:  

Cancer

BCPT02 (BLD1102) is a Topoisomerase-I inhibitor and ADC payload (ADC Payload). BCPT02 can form the ADC BCG041. BCPT02 is applicable to cancer-related research .
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Cat. No.: HY-12455
CAS No.: 118292-34-5
Duocarmycin A is an antitumor antibiotic and DNA alkylating agent with broad-spectrum antibacterial activity, which can serve as a payload for synthesizing antibody-drug conjugates (ADCs). Duocarmycin A selectively binds to the AT-rich minor groove of DNA, forms covalent adducts by alkylating the adenine N3 residue, thereby disrupting DNA structure and inhibiting its replication and transcription. Duocarmycin A induces apoptosis, sub-G1 phase accumulation and chromatin condensation, reduces the levels of pro-caspase-3/9, and induces p53-independent p21 expression. Duocarmycin A is widely used in the research of various malignancies, including leukemia, sarcoma, glioblastoma, as well as multiple solid tumor models such as lung cancer, breast cancer, and colorectal cancer .
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Cat. No.: HY-177285
CAS No.: 1161925-41-2
Target:  

Kinesin ADC Payloads

Research Areas:  

Cancer

NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs) .
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Cat. No.: HY-164429
CAS No.: 2418533-90-9
Target:  

Integrin Elastase

Research Areas:  

Cancer

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 .
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