Signaling Pathways
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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.
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Products Related to Signaling Pathways(40699)
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Semaglutide is an agonist of glucagon-like peptide 1 receptor (GLP-1R; EC50 = 6.2 pM in a reporter assay using BHK cells expressing the human receptor).
- GC91632Verrucarin HCAS: 29953-50-2Purity: >70.00%
Verrucarin H is a macrocyclic trichothecene mycotoxin that has been found in M. verrucaria.
- GC91639Ferrous trisglycinateCAS: 34369-82-9Purity: >95.00%
Ferrous trisglycinate is an iron amino acid chelate.
- GC91647Perfluoropropanesulfonic AcidCAS: 423-41-6Purity: >90.00%
Perfluoropropanesulfonic acid is a perfluoroalkyl substance (PFAS).
- GC916502-(Morpholin-4-yl)ethane-1-sulfonamideCAS: 4945-80-6Purity: >98.00%
2-(Morpholin-4-yl)ethane-1-sulfonamide is a byproduct in the synthesis of diazo compounds.
- GC91655N-Methylnuciferine (iodide)CAS: 53098-68-3Purity: >98.00%
N-Methylnuciferine is an aporphine alkaloid that has been found in A. cherimola and has diverse biological activities.
- GC916588(Z),11(Z),14(Z)-HeptadecatrienalCAS: 56797-44-5Purity: >98.00%
8(Z),11(Z),14(Z)-Heptadecatrienal is a polyunsaturated fatty aldehyde.
- GC91669m-isobutyl IbuprofenCAS: 66622-47-7Purity: >98.00%
m-isobutyl Ibuprofen is a potential impurity in commercial preparations of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor ibuprofen.
- GC91675Artepillin CCAS: 72944-19-5Purity: >95.00%
Artepillin C is a prenylated cinnamic acid that has been found in B. grisebachii and has diverse biological activities.
- GC916804-Acetamido AntipyrineCAS: 83-15-8Purity: >95.00%
4-Acetamido antipyrine (4-AAAP) is an active metabolite of the non-opioid analgesic and antipyretic prodrug metamizole .
- GC91681Loxoprofen-SRSCAS: 83648-76-4Purity: >98.00%
Loxoprofen-SRS is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 0.5 and 0.39 for recombinant human COX-1 and COX-2, respectively) and an active metabolite of the prodrug loxoprofen .
- GC91690TASP0277308CAS: 945725-50-8Purity: >98.00%
TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC91624 | 7-PPD-Q | 2894124-00-4 | >95.00% | |
7-PPD-Q is an oxidized derivative of the tire antiozonant and a substituted p-phenylenediamine 7-PPD. | ||||
| GC91627 | Semaglutide (sodium salt) | 2924330-56-1 | >98.00% | |
Semaglutide is an agonist of glucagon-like peptide 1 receptor (GLP-1R; EC50 = 6.2 pM in a reporter assay using BHK cells expressing the human receptor). | ||||
| GC91629 | OPPD-Q | 2952779-34-7 | >98.00% | |
OPPD-Q is a p-phenylenediamine-quinone (PPD-Q) and an oxidized derivative of the aromatic amine antioxidant OPPD . | ||||
| GC91632 | Verrucarin H | 29953-50-2 | >70.00% | |
Verrucarin H is a macrocyclic trichothecene mycotoxin that has been found in M. verrucaria. | ||||
| GC91634 | ARN25062 | 3036492-85-7 | >95.00% | |
ARN25062 is a derivative of ARN22089, an inhibitor of the protein-protein interaction between Cdc42 and p21-activated kinase (PAK). | ||||
| GC91639 | Ferrous trisglycinate | 34369-82-9 | >95.00% | |
Ferrous trisglycinate is an iron amino acid chelate. | ||||
| GC91647 | Perfluoropropanesulfonic Acid | 423-41-6 | >90.00% | |
Perfluoropropanesulfonic acid is a perfluoroalkyl substance (PFAS). | ||||
| GC91648 | Akt-I-1 | 473382-39-7 | >98.00% | |
Akt-I-1 is an inhibitor of Akt1 (IC50 = 4.6 µM). | ||||
| GC91650 | 2-(Morpholin-4-yl)ethane-1-sulfonamide | 4945-80-6 | >98.00% | |
2-(Morpholin-4-yl)ethane-1-sulfonamide is a byproduct in the synthesis of diazo compounds. | ||||
| GC91655 | N-Methylnuciferine (iodide) | 53098-68-3 | >98.00% | |
N-Methylnuciferine is an aporphine alkaloid that has been found in A. cherimola and has diverse biological activities. | ||||
| GC91658 | 8(Z),11(Z),14(Z)-Heptadecatrienal | 56797-44-5 | >98.00% | |
8(Z),11(Z),14(Z)-Heptadecatrienal is a polyunsaturated fatty aldehyde. | ||||
| GC91659 | BDW-OH | 573976-22-4 | >95.00% | |
BDW-OH is an active metabolite of the STING agonist and prodrug BDW568 . | ||||
| GC91660 | Alborixin | 57760-36-8 | >70.00% | |
Alborixin is an ionophore originally isolated from S. albus that has diverse biological activities. | ||||
| GC91667 | NSC 44625 | 654-62-6 | >98.00% | |
NSC 44625 is an inhibitor of carbonic anhydrase II (CAII; Ki = 63 nM for the human enzyme). | ||||
| GC91669 | m-isobutyl Ibuprofen | 66622-47-7 | >98.00% | |
m-isobutyl Ibuprofen is a potential impurity in commercial preparations of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor ibuprofen. | ||||
| GC91670 | MRSA Antibiotic 1 | 667410-81-3 | >95.00% | |
MRSA antibiotic 1 is an antibiotic. | ||||
| GC91672 | IPPD-Q | 68054-73-9 | >98.00% | |
IPPD-Q는 N,N'-Substituted p-phenylenediamines (PPD)의 산화 생성물로 디티오들글리톨(DTT) 소비율에 대한 산화 잠재력 값이 0.93μM min–1μM–1이다. IPPD-Q는 대기오염 연구와 오염물질 진단 연구에 사용되었다. | ||||
| GC91673 | CPPD-Q | 68054-78-4 | >98.00% | |
CPPD-Q is an oxidized derivative of the antioxidant CPPD, possessing antibacterial and insecticidal effects. | ||||
| GC91675 | Artepillin C | 72944-19-5 | >95.00% | |
Artepillin C is a prenylated cinnamic acid that has been found in B. grisebachii and has diverse biological activities. | ||||
| GC91680 | 4-Acetamido Antipyrine | 83-15-8 | >95.00% | |
4-Acetamido antipyrine (4-AAAP) is an active metabolite of the non-opioid analgesic and antipyretic prodrug metamizole . | ||||
| GC91681 | Loxoprofen-SRS | 83648-76-4 | >98.00% | |
Loxoprofen-SRS is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 0.5 and 0.39 for recombinant human COX-1 and COX-2, respectively) and an active metabolite of the prodrug loxoprofen . | ||||
| GC91688 | PDIC-NN | 932740-48-2 | >95.00% | |
PDIC-NN is an intermediate in the synthesis of PDIC-NS , an activator of stimulator of interferon genes (STING) with anticancer activity. | ||||
| GC91689 | TG46 | 936091-15-5 | >98.00% | |
TG46 is an inhibitor of JAK2 (IC50 = 12.5 µM). | ||||
| GC91690 | TASP0277308 | 945725-50-8 | >98.00% | |
TASP0277308 is a sphingosine-1-phosphate receptor 1 (S1P1) antagonist (IC50 = 4.2 nM). | ||||