Signaling Pathways
Research Area, Signaling Pathways | GlpBio Life Science Products Suppliers
Read More about this categoryShow Less
The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.
ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.
The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.
References:
[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.
[2] Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.
Research Areas
- Proteases(4889)
- Apoptosis(3387)
- Chromatin/Epigenetics(1950)
- Metabolism(3169)
- MAPK Signaling(740)
- Tyrosine Kinase(1639)
- DNA Damage/DNA Repair(2198)
- PI3K/Akt/mTOR Signaling(789)
- Microbiology & Virology(3936)
- Cell Cycle/Checkpoint(1546)
- Ubiquitination/ Proteasome(1418)
- JAK/STAT Signaling(578)
- TGF-β / Smad Signaling(398)
- Angiogenesis(417)
- GPCR/G protein(3755)
- Stem Cell(520)
- Membrane Transporter/Ion Channel(2495)
- Cancer Biology(589)
- Endocrinology and Hormones(1013)
- Neuroscience(4382)
- Obesity, Appetite Control & Diabetes(354)
- Peptide Inhibitors and Substrate(1)
- Other Signal Transduction(131)
- Immunology/Inflammation(4970)
- Cardiovascular(821)
- Vitamin D Related(78)
- PROTAC(337)
- Ox Stress Reagents(514)
- Others(4279)
- Antiparasitics(145)
- Toxins(85)
- Drug Derivative(182)
- OGA(1)
- Anti-infection(13)
- Metabolic Enzyme/Protease(29)
Products Related to Signaling Pathways(40876)
- GC12143Deltorphin ICAS: 122752-15-2Purity: >98.00%
La deltorfina I es un agonista del receptor opioide δ con alta afinidad y selectividad.
- GC12534ICI 199,441 hydrochlorideCAS: 115199-84-3Purity: >97.00%
El clorhidrato de ICI 199,441 es un agonista del receptor opioide &7#954 potente y selectivo.
- GC12663N-Benzylnaltrindole hydrochlorideCAS: 1206487-81-1Purity: >98.00%
δ2 opioid receptor antagonist
- GC12724Phenoxybenzamine HClCAS: 63-92-3Purity: >98.00%
El clorhidrato de fenoxibenzamina es un antagonista de los receptores adrenérgicos α, no selectivo, irreversible y activo por vÍa oral que se usa comÚnmente para la investigaciÓn de la hipertensiÓn, especÍficamente causada por el feocromocitoma.
- GC13103AZ505 ditrifluoroacetateCAS: 1035227-44-1Purity: >99.50%
El ditrifluoroacetato AZ505 es un inhibidor potente y selectivo de SMYD2 con IC50 de 0,12 μM.
- GC13546Dynorphin ACAS: 80448-90-4Purity: >98.50%
Dynorphin A es un péptido opioide endógeno que activa el canal receptor huérfano XOR1-K + , con un valor EC 50 de 45nM
- GC13581SB 205607 dihydrobromideCAS: 148545-09-9Purity: >98.00%
non-peptide δ1 opioid receptor agonist
- GC13645nor-Binaltorphimine dihydrochlorideCAS: 113158-34-2Purity: >99.50%
nor-Binaltorphimine dihydrochloride es un potente y selectivo antagonista del receptor opioide κ (KOR)
- GC13688Naltrindole hydrochlorideCAS: 111469-81-9Purity: >98.00%
El clorhidrato de naltrindol es un antagonista del receptor opioide no peptÍdico δ muy potente y selectivo con una Ki de 0,02 nM.
- GC13815Vinflunine TartrateCAS: 1201898-17-0Purity: >98.00%
Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis .
- GC14310NVP-ADW742CAS: 475488-23-4Purity: >99.00%
NVP-ADW742 (ADW742) es un inhibidor selectivo de la tirosina quinasa IGF-1R activo por vÍa oral con una IC50 de 0,17 μM.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC12143 | Deltorphin I | 122752-15-2 | >98.00% | |
La deltorfina I es un agonista del receptor opioide δ con alta afinidad y selectividad. | ||||
| GC12372 | SC-514 | 354812-17-2 | >99.50% | |
SC-514 es un inhibidor selectivo de IKK-2 (IC50=11,2 μM), que no inhibe otras isoformas de IKK ni otras serina-treonina y tirosina quinasas. | ||||
| GC12534 | ICI 199,441 hydrochloride | 115199-84-3 | >97.00% | |
El clorhidrato de ICI 199,441 es un agonista del receptor opioide &7#954 potente y selectivo. | ||||
| GC12548 | UNC 0631 | 1320288-19-4 | >99.00% | |
UNC 0631 es un potente inhibidor de la histona metiltransferasa G9a con una IC50 de 4 nM. UNC 0631 reduce de forma potente los niveles de H3K9me2 en células MDA-MB-231 con una IC50 de 25 nM. | ||||
| GC12663 | N-Benzylnaltrindole hydrochloride | 1206487-81-1 | >98.00% | |
δ2 opioid receptor antagonist | ||||
| GC12688 | (+)-U-50488 hydrochloride | 114528-81-3 | >98.00% | |
Selective κ-opioid agonist | ||||
| GC12724 | Phenoxybenzamine HCl | 63-92-3 | >98.00% | |
El clorhidrato de fenoxibenzamina es un antagonista de los receptores adrenérgicos α, no selectivo, irreversible y activo por vÍa oral que se usa comÚnmente para la investigaciÓn de la hipertensiÓn, especÍficamente causada por el feocromocitoma. | ||||
| GC13097 | ICI 204,448 hydrochloride | 121264-04-8 | >98.00% | |
κ opioid receptor agonist | ||||
| GC13103 | AZ505 ditrifluoroacetate | 1035227-44-1 | >99.50% | |
El ditrifluoroacetato AZ505 es un inhibidor potente y selectivo de SMYD2 con IC50 de 0,12 μM. | ||||
| GC13189 | Cyprodime hydrochloride | 118111-54-9 | - | |
μ-opioid receptor antagonist | ||||
| GC13393 | Epinephrine Bitartrate | 51-42-3 | >98.00% | |
Adrenergic receptor agonist | ||||
| GC13529 | CC-401 | 395104-30-0 | >98.00% | |
CC-401 es un potente inhibidor de las tres formas de JNK con Ki de 25 a 50 nM. | ||||
| GC13546 | Dynorphin A | 80448-90-4 | >98.50% | |
Dynorphin A es un péptido opioide endógeno que activa el canal receptor huérfano XOR1-K + , con un valor EC 50 de 45nM | ||||
| GC13581 | SB 205607 dihydrobromide | 148545-09-9 | >98.00% | |
non-peptide δ1 opioid receptor agonist | ||||
| GC13612 | PIK-294 | 900185-02-6 | >99.50% | |
PIK-294 es un potente inhibidor selectivo de p110δ con una IC50 de 10 nM. | ||||
| GC13645 | nor-Binaltorphimine dihydrochloride | 113158-34-2 | >99.50% | |
nor-Binaltorphimine dihydrochloride es un potente y selectivo antagonista del receptor opioide κ (KOR) | ||||
| GC13688 | Naltrindole hydrochloride | 111469-81-9 | >98.00% | |
El clorhidrato de naltrindol es un antagonista del receptor opioide no peptÍdico δ muy potente y selectivo con una Ki de 0,02 nM. | ||||
| GC13738 | SKLB1002 | 1225451-84-2 | >98.00% | |
VEGFR2 inhibitor,potent and ATP-competitve | ||||
| GC13744 | AZ505 | 1035227-43-0 | >99.50% | |
AZ505 es un inhibidor potente y selectivo de SMYD2 con una IC50 de 0,12 μM. | ||||
| GC13815 | Vinflunine Tartrate | 1201898-17-0 | >98.00% | |
Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis . | ||||
| GC13868 | GNE-9605 | 1536200-31-3 | >99.50% | |
GNE-9605 es un potente inhibidor selectivo de la cinasa repetida rica en leucina 2 (LRRK2), activo por vÍa oral, con un valor IC50 de 18,7 nM. | ||||
| GC13901 | AS-252424 | 900515-16-4 | >99.00% | |
AS-252424 es un inhibidor potente y selectivo de PI3Kγ con una IC50 de 30±10 nM. | ||||
| GC13910 | Salvinorin A | 83729-01-5 | >95.00% | |
Non-nitrogenous κ-opioid selective agonist | ||||
| GC14310 | NVP-ADW742 | 475488-23-4 | >99.00% | |
NVP-ADW742 (ADW742) es un inhibidor selectivo de la tirosina quinasa IGF-1R activo por vÍa oral con una IC50 de 0,17 μM. | ||||