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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| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GF05558 | Nigerose | 497-48-3 | >97.50% | |
Nigerose is a disaccharide composed of two glucose units linked by an α-1,3 glycosidic bond. | ||||
| GF05704 | Neochlorogenic acid methyl ester | 123410-65-1 | >98.00% | |
Neochlorogenic acid methyl ester is a compound with anti-HBV activity. | ||||
| GF10303 | Lipoteichoic acid | 56411-57-5 | - | |
Lipoteichoic acid is a teichoic acid predominantly located in the cell walls of Gram-positive bacteria, widely involved in stimulating immune responses and cellular signaling pathways. | ||||
| GF10446 | Keyhole limpet hemocyanin | 9013-72-3 | ≥85.00% | |
Keyhole limpet hemocyanin is a highly immunogenic copper-containing respiratory protein derived from the marine mollusk Megathura crenulata . | ||||
| GF10624 | Isohomoarbutin | 25162-30-5 | >98.00% | |
Isohomoarbutin is a phenolic compound isolated from the whole herb of Pyrola rotundifolia (Pyrolaceae) . | ||||
| GF11023 | Hecubine | 62874-52-6 | >98.00% | |
Hecubine is a natural aspidosperma-type alkaloid found in E. officinalis , with anti-neuroinflammation properties. | ||||
| GF14666 | D-Glucosamine 6-phosphate | 3616-42-0 | >98.00% | |
D-Glucosamine 6-phosphate is an endogenous metabolite, a phosphorylated form of glucosamine, which can be synthesized by glutamine fructose-6-phosphate aminotransferase (GFAT). | ||||
| GF15486 | Cathepsin B from bovine spleen | 9047-22-7 | - | |
Cathepsin B from bovine spleen (Cathepsin B) is a member of the cysteine protease papain-like family. Cathepsin B is synthesized as a preproenzyme consisting of 335 amino acids, with a calculated molecular weight of approximately 36.7kDa. Cathepsin B is localized in the endosomal/lysosomal compartment, where Cathepsin B functions as both an endopeptidase and an exopeptidase. Cathepsin B primarily participates in the routine turnover of intracellular and extracellular proteins, thereby maintaining the homeostatic metabolic activity within the cell. | ||||
| GF17531 | 8-Epixanthatin | 30890-35-8 | >98.00% | |
8-Epixanthatin is a light-induced growth inhibitor that regulates the phototropic curvature in sunflower hypocotyls. | ||||
| GF20672 | 5α-Androstanedione | 846-46-8 | >98.00% | |
5α-Androstanedione is an endogenous steroid hormone metabolite and a key intermediate. | ||||
| GF44560 | 11β,13-Dihydrotaraxinic acid β-D-glucopyranosyl ester | 75911-16-9 | >98.00% | |
11β,13-Dihydrotaraxinic acid β-D-glucopyranosyl ester is a eudesmane-type (germacranolide-derived) sesquiterpene lactone glucopyranosyl ester isolated from Taraxacum officinale , and 11β,13-Dihydrotaraxinic acid β-D-glucopyranosyl ester exhibits relatively low cytotoxicity toward cells. | ||||
| GN10001 | Sennoside A | 81-27-6 | >99.00% | |
| GN10004 | EsculentosideA | 65497-07-6 | >99.50% | |
| GN10005 | Schisandrin C | 61301-33-5 | >99.50% | |
| GN10006 | 3,4-Dihydroxybenzaldehyde | 139-85-5 | >99.50% | |
| GN10008 | Reutericyclin | 303957-69-9 | >98.00% | |
A small molecular weight antibiotic isolated from Lactobacillus reuteri | ||||
| GN10011 | Rebaudioside A | 58543-16-1 | >98.00% | |
Rebaudioside A, from leaves of Stevia rebaudiana , inhibits α-glucosidase activity with IC 50 =35.01μg/ml. | ||||
| GN10015 | Corosolic Acid | 4547-24-4 | >98.00% | |
| GN10016 | Carnosol | 5957-80-2 | >98.00% | |
| GN10017 | Wogonin | 632-85-9 | >98.00% | |
Wogonin is a potent and competitive inhibitor of CYP1A2 with a K i value of 0.24μM. | ||||
| GN10018 | Baicalin | 21967-41-9 | >98.00% | |
Baicalin is a flavonoid glycoside and an allosteric carnitine palmitoyltransferase 1 (CPT1) activator. | ||||
| GN10019 | Ginsenoside Rg6 | 147419-93-0 | >99.50% | |
| GN10020 | Piperine | 94-62-2 | >98.00% | |
| GN10022 | luteolin-6-C-glucoside | 4261-42-1 | >98.00% | |