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(4888)
- Apoptosis(3381)
- Chromatin/Epigenetics(1948)
- Metabolism(3165)
- MAPK Signaling(739)
- Tyrosine Kinase(1637)
- DNA Damage/DNA Repair(2193)
- PI3K/Akt/mTOR Signaling(786)
- Microbiology & Virology(3931)
- Cell Cycle/Checkpoint(1540)
- Ubiquitination/ Proteasome(1416)
- JAK/STAT Signaling(577)
- TGF-β / Smad Signaling(397)
- Angiogenesis(415)
- GPCR/G protein(3749)
- Stem Cell(518)
- Membrane Transporter/Ion Channel(2493)
- Cancer Biology(589)
- Endocrinology and Hormones(1012)
- Neuroscience(4379)
- Obesity, Appetite Control & Diabetes(354)
- Peptide Inhibitors and Substrate(1)
- Other Signal Transduction(131)
- Immunology/Inflammation(4960)
- Cardiovascular(821)
- Vitamin D Related(78)
- PROTAC(336)
- Ox Stress Reagents(514)
- Others(4278)
- Antiparasitics(145)
- Toxins(85)
- Drug Derivative(182)
- OGA(1)
- Anti-infection(12)
- Metabolic Enzyme/Protease(21)
Products Related to Signaling Pathways(40823)
- GC91530β-Ionone AcidCAS: 14393-45-4Purity: >98.00%
β-Ionone acid is the acid form of the β-carotenoid derivative β-ionone.
- GC915405-Acetamide-ButenolideCAS: 16275-44-8Purity: >70.00%
5-Acetamide-butenolide is a mycotoxin that has been found in Fusarium and has pro-oxidant activity.
- GC91543(E/Z)-DroloxifeneCAS: 165813-01-4Purity: >98.00%
(E/Z)-Droloxifene is a mixture of (E)-droloxifene, a selective estrogen receptor modulator (SERM), and (Z)-droloxifene.
- GC91544Fmoc-L-Lys[Oct-(OtBu)-Glu-(OtBu)-AEEA-AEEA]-OHCAS: 1662688-20-1Purity: >99.50%
Fmoc-L-Lys[Oct-(OtBu)-Glu-(OtBu)-AEEA-AEEA]-OH is a building block in the synthesis of the glucagon-like peptide 1 receptor (GLP-1R) agonist semaglutide .
- GC91547Tanzawaic Acid BCAS: 169181-33-3Purity: >70.00%
Tanzawaic acid B is a fungal metabolite that has been found in Penicillium and has diverse biological activities.
- GC91548Rosuvastatin EP Impurity A (calcium salt)CAS: 1714147-47-3Purity: >98.00%
Rosuvastatin EP impurity A is a potential impurity in commercial preparations of the HMG-CoA reductase inhibitor rosuvastatin.
- GC91549L-742,001 (hydrochloride)CAS: 174605-64-2Purity: >98.00%
L-742,001 is an inhibitor of influenza virus PA endonuclease (IC50 = 0.5 µM), an essential subdomain of the viral RNA polymerase.
- GC91565GSK199 analog (hydrochloride)CAS: 2048226-46-4Purity: >95.00%
GSK199 analog is an inhibitor of peptidyl arginine deiminase 4 (PAD4) and a derivative of the PAD4 inhibitor GSK199.
- GC9158110-(Phosphonooxy)-1-decanoleCAS: 235097-47-9Purity: >98.00%
10-(Phosphonooxy)-1-decanole is a hydrolytic degradation product of 10-methacryloyloxydecyl dihydrogen phosphate-N-methylacryloyl glycine (MDP-NMGly) dental primers.
- GC91583ClerosterolCAS: 2364-23-0Purity: >95.00%
Clerosterol is a phytosterol that has been found in C. fragile and has diverse biological activities.
- GC9158510α-hydroxy NaltrexoneCAS: 2397651-97-5Purity: >95.00%
10α-hydroxy Naltrexone is a derivative of the opioid antagonist naltrexone.
- GC91594LYS-006 (hydrochloride)CAS: 2619563-79-8Purity: >98.00%
LYS-006 is an inhibitor of leukotriene A4 (LTA4) hydrolase.
- GC91603Homogentisic Acid lactoneCAS: 2688-48-4Purity: >95.00%
Homogentisic acid lactone is a fungal metabolite that has been found in the fungus WF5, has fungicidal activity, and is the lactonized form of homogentisic acid , an intermediate in aromatic amino acid metabolism.
- GC91613FerroLOXIN-1CAS: 2773428-48-9Purity: >90.00%
FerroLOXIN-1 is an inhibitor of the 15-lipoxygenase-2 (15-LO-2) and phosphatidylethanolamine-binding protein 1 (PEBP1) catalytic complex.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC91530 | β-Ionone Acid | 14393-45-4 | >98.00% | |
β-Ionone acid is the acid form of the β-carotenoid derivative β-ionone. | ||||
| GC91533 | DTPD | 15017-02-4 | >99.50% | |
DTPD is a substituted p-phenylenediamine and non-oxidized version of DTPD-Q . | ||||
| GC91540 | 5-Acetamide-Butenolide | 16275-44-8 | >70.00% | |
5-Acetamide-butenolide is a mycotoxin that has been found in Fusarium and has pro-oxidant activity. | ||||
| GC91543 | (E/Z)-Droloxifene | 165813-01-4 | >98.00% | |
(E/Z)-Droloxifene is a mixture of (E)-droloxifene, a selective estrogen receptor modulator (SERM), and (Z)-droloxifene. | ||||
| GC91544 | Fmoc-L-Lys[Oct-(OtBu)-Glu-(OtBu)-AEEA-AEEA]-OH | 1662688-20-1 | >99.50% | |
Fmoc-L-Lys[Oct-(OtBu)-Glu-(OtBu)-AEEA-AEEA]-OH is a building block in the synthesis of the glucagon-like peptide 1 receptor (GLP-1R) agonist semaglutide . | ||||
| GC91547 | Tanzawaic Acid B | 169181-33-3 | >70.00% | |
Tanzawaic acid B is a fungal metabolite that has been found in Penicillium and has diverse biological activities. | ||||
| GC91548 | Rosuvastatin EP Impurity A (calcium salt) | 1714147-47-3 | >98.00% | |
Rosuvastatin EP impurity A is a potential impurity in commercial preparations of the HMG-CoA reductase inhibitor rosuvastatin. | ||||
| GC91549 | L-742,001 (hydrochloride) | 174605-64-2 | >98.00% | |
L-742,001 is an inhibitor of influenza virus PA endonuclease (IC50 = 0.5 µM), an essential subdomain of the viral RNA polymerase. | ||||
| GC91565 | GSK199 analog (hydrochloride) | 2048226-46-4 | >95.00% | |
GSK199 analog is an inhibitor of peptidyl arginine deiminase 4 (PAD4) and a derivative of the PAD4 inhibitor GSK199. | ||||
| GC91574 | (±)2-HOTrE | 22324-71-6 | >98.00% | |
(±)2-HOTrE is an oxylipin. | ||||
| GC91576 | Nedometinib | 2252314-46-6 | >98.00% | |
Nedometinib is a MEK1 inhibitor (IC50 = 135 nM). | ||||
| GC91581 | 10-(Phosphonooxy)-1-decanole | 235097-47-9 | >98.00% | |
10-(Phosphonooxy)-1-decanole is a hydrolytic degradation product of 10-methacryloyloxydecyl dihydrogen phosphate-N-methylacryloyl glycine (MDP-NMGly) dental primers. | ||||
| GC91583 | Clerosterol | 2364-23-0 | >95.00% | |
Clerosterol is a phytosterol that has been found in C. fragile and has diverse biological activities. | ||||
| GC91585 | 10α-hydroxy Naltrexone | 2397651-97-5 | >95.00% | |
10α-hydroxy Naltrexone is a derivative of the opioid antagonist naltrexone. | ||||
| GC91590 | DTPD-Q | 252950-56-4 | >98.00% | |
DTPD-Q is an oxidized derivative of the antioxidant and methylphenyl substituted p-phenylenediamine DTPD. | ||||
| GC91592 | CP-4 | 2569194-72-3 | >98.00% | |
CP-4 is a fluorescent probe for mesenchymal stem cells. | ||||
| GC91594 | LYS-006 (hydrochloride) | 2619563-79-8 | >98.00% | |
LYS-006 is an inhibitor of leukotriene A4 (LTA4) hydrolase. | ||||
| GC91595 | PDIC-NC | 2633013-75-7 | >95.00% | |
PDIC-NC is an activator of stimulator of interferon genes (STING) and an anticancer agent. | ||||
| GC91598 | GPX4 16 | 2644044-43-7 | >98.00% | |
GPX4 16 is an inhibitor of glutathione peroxidase 4 (GPX4). | ||||
| GC91602 | PFI-6 | 2675452-91-0 | >95.00% | |
PFI-6 is a chemical probe for the YEATS domain-containing proteins MLLT1 and MLLT3 (IC50s = 140 and 160 nM, respectively). | ||||
| GC91603 | Homogentisic Acid lactone | 2688-48-4 | >95.00% | |
Homogentisic acid lactone is a fungal metabolite that has been found in the fungus WF5, has fungicidal activity, and is the lactonized form of homogentisic acid , an intermediate in aromatic amino acid metabolism. | ||||
| GC91604 | 8RK64 | 2705841-52-5 | >95.00% | |
8RK64 is a covalent inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1; IC50 = 0.32 µM) and a click chemistry reagent. | ||||
| GC91612 | FDW028 | 2768426-49-7 | >98.00% | |
FDW028 is an inhibitor of fucosyltransferase 8 (FUC8). | ||||
| GC91613 | FerroLOXIN-1 | 2773428-48-9 | >90.00% | |
FerroLOXIN-1 is an inhibitor of the 15-lipoxygenase-2 (15-LO-2) and phosphatidylethanolamine-binding protein 1 (PEBP1) catalytic complex. | ||||