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(40698)
- GC81775Cedrol methyl etherCAS: 19870-74-7Purity: >98.00%
Cedrol methyl ether is an active ingredient that can be extracted from ginger.
- GC817765-Hydroxytryptophol-O-glucuronideCAS: 27939-38-4Purity: >99.50%
5-Hydroxytryptophol-O-glucuronide (UGT1A6) is an authentic glucuronide standard and probe metabolite.
- GC81777ABS-752 hydrochlorideCAS: 2922884-90-8Purity: >98.50%
ABS-752 hydrochloride is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation.
- GC81785Protocatechuic acid-2-glucosideCAS: 3056651-89-6Purity: >98.00%
Protocatechuic acid-2-glucoside (compound 6) is a phenolic acid glycoside.
- GC81788(2R)-Naringenin-5-O-β-D-glucopyranosideCAS: 19253-00-0Purity: >98.00%
(2R)-Naringenin-5-O-β-D-glucopyranoside (Compound 4) is a flavonoid glucoside found in the aerial parts of Helichrysum zivojinii [1] .
- GC81800Betavulgaroside IIICAS: 168111-48-6Purity: >98.00%
Betavulgaroside III is a triterpene seco-glycoside plant saponin.
- GC818171-Phenylethanamine-d₃ hydrochloridePurity: >98.00%
1-Phenylethanamine-d 3 hydrochloride is the deuterated-labeled 1-Phenylethanamine hydrochloride.
- GC8181811β,13-DihydrolactucopicrinCAS: 125519-47-3Purity: >98.00%
11β,13-Dihydrolactucopicrin is a sesquiterpene lactone and the main bitter component of chicory root.
- GC818224-Chloro-N-methylpicolinamide-d₃CAS: 1189858-48-7Purity: >98.00%
4-Chloro-N-methylpicolinamide -d 3 is the deuterated-labeled 4-Chloro-N-methylpicolinamide.
- GC81826β-EpoxysitosterolCAS: 20835-90-9Purity: >98.00%
β-Epoxysitosterol is an Estrogen receptor α agonist.
- GC81827Buforin IIb TFAPurity: >98.00%
Buforin IIb TFA (BF2-B TFA) is an anticancer peptide, as well as an Antibacterial and Antifungal agent.
- GC81832E3 ligase Ligand 64-2-(4-hydroxypiperidin-4-yl)acetic acidCAS: 2654826-81-8Purity: >98.00%
E3 ligase Ligand 64-2-(4-hydroxypiperidin-4-yl) acetic acid is an E3 ligase-linker conjugate.
- GC81833Ethylmalonyl-CoA pentalithiumPurity: >98.00%
Ethylmalonyl-CoA pentalithium (Ethylmalonyl coenzyme A pentalithium) is a metabolic intermediate and biosynthetic precursor associated with crotonyl-CoA carboxylase/reductase.
- GC81834F3 peptide acetatePurity: >98.00%
F3 peptide acetate is a nucleolin-binding tumor-homing peptide that mediates selective uptake and internalization by tumor cells.
- GC81836H-D-Val-Leu-Lys-AFC TFAPurity: >98.50%
H-D-Val-Leu-Lys-AFC TFA (Plasmin substrate TFA) is a plasmin -specific fluorescent substrate.
- GC81837Histone H4 peptide substrate (1-21) acetatePurity: >98.00%
Histone H4 peptide substrate (1-21) acetate is a PAD4 peptide substrate.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81775 | Cedrol methyl ether | 19870-74-7 | >98.00% | |
Cedrol methyl ether is an active ingredient that can be extracted from ginger. | ||||
| GC81776 | 5-Hydroxytryptophol-O-glucuronide | 27939-38-4 | >99.50% | |
5-Hydroxytryptophol-O-glucuronide (UGT1A6) is an authentic glucuronide standard and probe metabolite. | ||||
| GC81777 | ABS-752 hydrochloride | 2922884-90-8 | >98.50% | |
ABS-752 hydrochloride is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. | ||||
| GC81778 | LATS-IN-2 | 2248728-49-4 | >99.00% | |
LATS-IN-2 is an efficiently acting LATS ( large tumor suppressor kinase) inhibitor. | ||||
| GC81785 | Protocatechuic acid-2-glucoside | 3056651-89-6 | >98.00% | |
Protocatechuic acid-2-glucoside (compound 6) is a phenolic acid glycoside. | ||||
| GC81788 | (2R)-Naringenin-5-O-β-D-glucopyranoside | 19253-00-0 | >98.00% | |
(2R)-Naringenin-5-O-β-D-glucopyranoside (Compound 4) is a flavonoid glucoside found in the aerial parts of Helichrysum zivojinii [1] . | ||||
| GC81800 | Betavulgaroside III | 168111-48-6 | >98.00% | |
Betavulgaroside III is a triterpene seco-glycoside plant saponin. | ||||
| GC81801 | Neocrocin B | 2001062-74-2 | >95.00% | |
Neocrocin B is a carotenoid crocin. | ||||
| GC81812 | (S)-N-(4-((3-Methoxy-4-(2-methyl-2H-1,2,3-triazol-4-yl)pyridin-2-yl)amino)-5-propionylpyridin-2-yl)spiro[2.2]pentane-1-carboxamide-d 3 | 3062086-74-9 | >98.00% | |
| GC81817 | 1-Phenylethanamine-d₃ hydrochloride | - | >98.00% | |
1-Phenylethanamine-d 3 hydrochloride is the deuterated-labeled 1-Phenylethanamine hydrochloride. | ||||
| GC81818 | 11β,13-Dihydrolactucopicrin | 125519-47-3 | >98.00% | |
11β,13-Dihydrolactucopicrin is a sesquiterpene lactone and the main bitter component of chicory root. | ||||
| GC81822 | 4-Chloro-N-methylpicolinamide-d₃ | 1189858-48-7 | >98.00% | |
4-Chloro-N-methylpicolinamide -d 3 is the deuterated-labeled 4-Chloro-N-methylpicolinamide. | ||||
| GC81824 | (+)-Talinolol | 71369-60-3 | >99.00% | |
(+)-Talinolol is an isomer of Talinolol. | ||||
| GC81825 | ASO-4625 | - | >98.00% | |
ASO-4625 is a 20-nucleotide gapmer antisense oligonucleotide with a full phosphorothioate backbone and 2'-O-(2-methoxy) ethyl ribose modifications, which targets BCL2 mRNA and BCL2L1 mRNA. | ||||
| GC81826 | β-Epoxysitosterol | 20835-90-9 | >98.00% | |
β-Epoxysitosterol is an Estrogen receptor α agonist. | ||||
| GC81827 | Buforin IIb TFA | - | >98.00% | |
Buforin IIb TFA (BF2-B TFA) is an anticancer peptide, as well as an Antibacterial and Antifungal agent. | ||||
| GC81830 | D-RGDW acetate | - | >98.00% | |
D-RGDW acetate is an Arg-Gly-Asp (RGD) containing peptide. | ||||
| GC81832 | E3 ligase Ligand 64-2-(4-hydroxypiperidin-4-yl)acetic acid | 2654826-81-8 | >98.00% | |
E3 ligase Ligand 64-2-(4-hydroxypiperidin-4-yl) acetic acid is an E3 ligase-linker conjugate. | ||||
| GC81833 | Ethylmalonyl-CoA pentalithium | - | >98.00% | |
Ethylmalonyl-CoA pentalithium (Ethylmalonyl coenzyme A pentalithium) is a metabolic intermediate and biosynthetic precursor associated with crotonyl-CoA carboxylase/reductase. | ||||
| GC81834 | F3 peptide acetate | - | >98.00% | |
F3 peptide acetate is a nucleolin-binding tumor-homing peptide that mediates selective uptake and internalization by tumor cells. | ||||
| GC81835 | G4232 | - | >98.00% | |
G4232 is an immune-silent BCL2 antisense oligonucleotide that binds to BCL2 mRNA to induce target degradation and inhibit Bcl-2 protein translation. | ||||
| GC81836 | H-D-Val-Leu-Lys-AFC TFA | - | >98.50% | |
H-D-Val-Leu-Lys-AFC TFA (Plasmin substrate TFA) is a plasmin -specific fluorescent substrate. | ||||
| GC81837 | Histone H4 peptide substrate (1-21) acetate | - | >98.00% | |
Histone H4 peptide substrate (1-21) acetate is a PAD4 peptide substrate. | ||||
| GC81838 | ICA604025 | - | >98.00% | |
ICA604025 is a state-dependent inhibitor of human Nav1.9 voltage-gated sodium channel. | ||||