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(38391)
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El clorhidrato de naltrindol es un antagonista del receptor opioide no peptÍdico δ muy potente y selectivo con una Ki de 0,02 nM.
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Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis .
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NVP-ADW742 (ADW742) es un inhibidor selectivo de la tirosina quinasa IGF-1R activo por vÍa oral con una IC50 de 0,17 μM.
- GC15062Ki16198CAS: 355025-13-7Purity: >98.50%
Ki16198 es un antagonista del receptor LPA potente y activo por vÍa oral, el éster metÍlico de Ki16425. Ki16198 inhibe la producciÓn de fosfato de inositol inducida por LPA1 y LPA3 con valores de Ki de 0,34 μM y 0,93 μM, respectivamente. Ki16198 es eficaz para la tumorigénesis y la metÁstasis del cÁncer de pÁncreas in vivo.
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κ/μ opioid receptor agonist,potent and selective
- GC15480Marinopyrrole ACAS: 1227962-62-0Purity: >99.50%
El marinopirrol A (Marinopirrol A) es un inhibidor de Mcl-1 novedoso y especÍfico con un valor IC50 de 10,1 μM, y muestra una selectividad >8 veces mayor que BCL-xl (IC50 > 80 μM).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC13581 | SB 205607 dihydrobromide | 148545-09-9 | >98% | |
non-peptide δ1 opioid receptor agonist | ||||
| GC13612 | PIK-294 | 900185-02-6 | >99.50% | |
PIK-294 es un potente inhibidor selectivo de p110δ con una IC50 de 10 nM. | ||||
| GC13645 | nor-Binaltorphimine dihydrochloride | 113158-34-2 | >99.50% | |
nor-Binaltorphimine dihydrochloride es un potente y selectivo antagonista del receptor opioide κ (KOR) | ||||
| GC13688 | Naltrindole hydrochloride | 111469-81-9 | >98% | |
El clorhidrato de naltrindol es un antagonista del receptor opioide no peptÍdico δ muy potente y selectivo con una Ki de 0,02 nM. | ||||
| GC13738 | SKLB1002 | 1225451-84-2 | >98% | |
VEGFR2 inhibitor,potent and ATP-competitve | ||||
| GC13744 | AZ505 | 1035227-43-0 | >99.50% | |
AZ505 es un inhibidor potente y selectivo de SMYD2 con una IC50 de 0,12 μM. | ||||
| GC13815 | Vinflunine Tartrate | 1201898-17-0 | >98% | |
Etanercept is an inhibitor of the inflammatory factor TNF-α and is mainly used for the clinical treatment of rheumatoid arthritis . | ||||
| GC13868 | GNE-9605 | 1536200-31-3 | >99.50% | |
GNE-9605 es un potente inhibidor selectivo de la cinasa repetida rica en leucina 2 (LRRK2), activo por vÍa oral, con un valor IC50 de 18,7 nM. | ||||
| GC13901 | AS-252424 | 900515-16-4 | >99.00% | |
AS-252424 es un inhibidor potente y selectivo de PI3Kγ con una IC50 de 30±10 nM. | ||||
| GC13910 | Salvinorin A | 83729-01-5 | >95.00% | |
Non-nitrogenous κ-opioid selective agonist | ||||
| GC14310 | NVP-ADW742 | 475488-23-4 | >99.00% | |
NVP-ADW742 (ADW742) es un inhibidor selectivo de la tirosina quinasa IGF-1R activo por vÍa oral con una IC50 de 0,17 μM. | ||||
| GC14318 | CAY10505 | 1218777-13-9 | >99.50% | |
CAY10505 es un inhibidor potente y selectivo de PI3Kγ con una IC50 de 30 nM en neuronas. | ||||
| GC14525 | ML 190 | 1355244-02-8 | >98% | |
ML 190 es un antagonista selectivo del receptor opioide κ (KOR) con una IC50 de 120 nM y una EC50 de 129 nM, respectivamente. | ||||
| GC14739 | GR 89696 fumarate | 126766-32-3 | >98% | |
κ-opioid agonist | ||||
| GC14774 | DSLET | 75644-90-5 | >98% | |
δ Opioid receptor agonist | ||||
| GC14868 | Milrinone | 78415-72-2 | >99.50% | |
La milrinona es un inhibidor de la PDE3 y también un inotrÓpico y vasodilatador. | ||||
| GC14979 | N-MPPP Hydrochloride | 207452-97-9 | >98% | |
High affinity κ agonist | ||||
| GC15035 | PM00104 | 308359-57-1 | >98% | |
Potent antimyeloma agent | ||||
| GC15062 | Ki16198 | 355025-13-7 | >98.50% | |
Ki16198 es un antagonista del receptor LPA potente y activo por vÍa oral, el éster metÍlico de Ki16425. Ki16198 inhibe la producciÓn de fosfato de inositol inducida por LPA1 y LPA3 con valores de Ki de 0,34 μM y 0,93 μM, respectivamente. Ki16198 es eficaz para la tumorigénesis y la metÁstasis del cÁncer de pÁncreas in vivo. | ||||
| GC15078 | Dynorphin B | 83335-41-5 | >98% | |
endogenous agonist for the kappa opioid receptor | ||||
| GC15179 | Ketorolac | 74103-06-3 | >98% | |
El ketorolaco (RS37619) es un fÁrmaco antiinflamatorio no esteroideo (AINE) que actÚa como un inhibidor no selectivo de la COX, con IC50 de 20 nM para COX-1 y 120 nM para COX-2. | ||||
| GC15313 | BRL 52537 hydrochloride | 112282-24-3 | >98% | |
κ/μ opioid receptor agonist,potent and selective | ||||
| GC15480 | Marinopyrrole A | 1227962-62-0 | >99.50% | |
El marinopirrol A (Marinopirrol A) es un inhibidor de Mcl-1 novedoso y especÍfico con un valor IC50 de 10,1 μM, y muestra una selectividad >8 veces mayor que BCL-xl (IC50 > 80 μM). | ||||
| GC15715 | AZD3839 | 1227163-56-5 | - | |
BACE1 inhibitor,potent and selective | ||||