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(40823)
- GC79784MAO-B-IN-55CAS: 1458219-02-7Purity: >98.00%
MAO-B-IN-55 (Compound 5c) is a reversible competitive MAO-B inhibitor with an IC 50 of 2.9 nM, and it exhibits approximately 2750-fold higher selectivity for MAO-B over MAO-A.
- GC797854-ChlorochalconeCAS: 956-04-7Purity: >98.00%
4-Chlorochalcone (Compound 3) is a monoamine oxidase inhibitor (hMAO-B: IC 50 = 0.082 μM, hMAO-A: IC 50 = 9.95 μM).
- GC79787Ac-IEAR-pNACAS: 132567-18-1Purity: >99.50%
Ac-IEAR-pNA is the chromogenic substrate for quantifying endotoxin levels.
- GC79791TrkA/NGF-IN-1CAS: 3105660-96-3Purity: >98.00%
TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF ( IC 50 : 21 nM for human TrkA in PathHunter assay).
- GC79795JNJ-64326067CAS: 2173357-28-1Purity: >98.00%
JNJ-64326067 is an aggregated tau-binding agent with blood-brain barrier permeability, with a K i of 2.4 nM.
- GC79796(E/Z)-FlorzolotauPurity: >98.00%
(E/Z)-Florzolotau ((E/Z)-APN1607) is a mixed configuration or unspecified configuration of Florzolotau.
- GC79798RI-AG03 acetatePurity: >98.00%
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy.
- GC79799trans-SobrerolCAS: 42370-41-2Purity: >99.50%
trans-Sobrerol (NRM-331) is a potent mucofluidifying agent.
- GC79800NucresiranPurity: >97.00%
Nucresiran is a siRNA that inhibits hepatic synthesis of both wild-type and variant TTR mRNA.
- GC79801α-Synuclein-IN-17CAS: 676458-63-2Purity: >98.00%
α-Synuclein-IN-17 (Compound 10) is an α-Synuclein inhibitor, with an IC 50 value of 9 μM.
- GC79803Paeonolsilate sodiumCAS: 827610-11-7Purity: >98.00%
Paeonolsilate (sodium) can inhibit ox-LDL-induced macrophage foam cell formation and inflammation in atherosclerosis.
- GC798056-MethoxymelleinCAS: 13410-15-6Purity: >99.00%
6-Methoxymellein, a phytoalexin, is a NF-κB inhibitor.
- GC79807RP-182 acetatePurity: >98.50%
RP-182 acetate is a synthetic immunomodulatory peptide that exerts anti-tumor effects by targeting the mannose receptor CD206 ( K d = 8 μM) on the surface of tumor-associated macrophages (TAMs).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC79784 | MAO-B-IN-55 | 1458219-02-7 | >98.00% | |
MAO-B-IN-55 (Compound 5c) is a reversible competitive MAO-B inhibitor with an IC 50 of 2.9 nM, and it exhibits approximately 2750-fold higher selectivity for MAO-B over MAO-A. | ||||
| GC79785 | 4-Chlorochalcone | 956-04-7 | >98.00% | |
4-Chlorochalcone (Compound 3) is a monoamine oxidase inhibitor (hMAO-B: IC 50 = 0.082 μM, hMAO-A: IC 50 = 9.95 μM). | ||||
| GC79786 | AAKLVFF | 1038400-67-7 | >99.50% | |
AAKLVFF is an oligopeptide capable of self-assembling into nanotubes. | ||||
| GC79787 | Ac-IEAR-pNA | 132567-18-1 | >99.50% | |
Ac-IEAR-pNA is the chromogenic substrate for quantifying endotoxin levels. | ||||
| GC79788 | BTA-1_b | 95856-73-8 | >98.00% | |
BTA-1 _b (BTA-1-CH3) is a structural analog of BTA-1. | ||||
| GC79789 | GZ-389988 | 1788906-96-6 | >99.00% | |
GZ-389988 is a potent pan-TRK inhibitor with IC 50 values of 0.3, 0.1, and 0.5 nM for TRKA, TRKB, and TRKC, respectively. | ||||
| GC79790 | A6CDQ | 1005550-46-8 | >98.00% | |
A6CDQ is a human organic cation transporter ( hOCT ) inhibitor with antidepressant-like activity that can cross the blood-brain barrier. | ||||
| GC79791 | TrkA/NGF-IN-1 | 3105660-96-3 | >98.00% | |
TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF ( IC 50 : 21 nM for human TrkA in PathHunter assay). | ||||
| GC79792 | (7RS)-Nivegacetor | - | >98.50% | |
(7RS)-Nivegacetor is the racemate of Nivegacetor. | ||||
| GC79793 | AZ1136 | 1380508-60-0 | >98.00% | |
AZ1136 is a γ-secretase modulator that regulates amyloid-β ( Aβ ) production without reducing total Aβ generation. | ||||
| GC79794 | Dopegal | 13023-73-9 | >98.00% | |
Dopegal is a metabolite od Norepinephrine. | ||||
| GC79795 | JNJ-64326067 | 2173357-28-1 | >98.00% | |
JNJ-64326067 is an aggregated tau-binding agent with blood-brain barrier permeability, with a K i of 2.4 nM. | ||||
| GC79796 | (E/Z)-Florzolotau | - | >98.00% | |
(E/Z)-Florzolotau ((E/Z)-APN1607) is a mixed configuration or unspecified configuration of Florzolotau. | ||||
| GC79797 | TAU-IN-6 | 3083792-74-6 | >98.00% | |
TAU-IN-6 (Compound 13) is a Tau protein misfolding and aggregation inhibitor. | ||||
| GC79798 | RI-AG03 acetate | - | >98.00% | |
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. | ||||
| GC79799 | trans-Sobrerol | 42370-41-2 | >99.50% | |
trans-Sobrerol (NRM-331) is a potent mucofluidifying agent. | ||||
| GC79800 | Nucresiran | - | >97.00% | |
Nucresiran is a siRNA that inhibits hepatic synthesis of both wild-type and variant TTR mRNA. | ||||
| GC79801 | α-Synuclein-IN-17 | 676458-63-2 | >98.00% | |
α-Synuclein-IN-17 (Compound 10) is an α-Synuclein inhibitor, with an IC 50 value of 9 μM. | ||||
| GC79802 | MODAG-005 | 2648041-73-8 | >98.00% | |
MODAG-005 is a blood-brain barrier-permeable PET probe precursor for α-synuclein ( α‑Syn ) aggregates, with a K i value of 0.4 nM and a K d value of 0.2 nM. | ||||
| GC79803 | Paeonolsilate sodium | 827610-11-7 | >98.00% | |
Paeonolsilate (sodium) can inhibit ox-LDL-induced macrophage foam cell formation and inflammation in atherosclerosis. | ||||
| GC79804 | Cupabimod | 297774-48-2 | >91.00% | |
Cupabimod is a decoy oligodeoxynucleotide for transcription factor NF-κB. | ||||
| GC79805 | 6-Methoxymellein | 13410-15-6 | >99.00% | |
6-Methoxymellein, a phytoalexin, is a NF-κB inhibitor. | ||||
| GC79806 | TKL002 | 3098518-95-4 | >98.00% | |
TKL002 is a blood-brain barrier-permeable inhibitor of the CTH/H 2 S/NF-κB/EMT signaling axis. | ||||
| GC79807 | RP-182 acetate | - | >98.50% | |
RP-182 acetate is a synthetic immunomodulatory peptide that exerts anti-tumor effects by targeting the mannose receptor CD206 ( K d = 8 μM) on the surface of tumor-associated macrophages (TAMs). | ||||