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(40938)
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(Rac)-δ-Viniferin is a racemate of δ-Viniferin, an isomer of ε-Viniferin.
- GC79591(1R)-BMS-986408CAS: 2618418-11-2Purity: >99.00%
(1R)-BMS-986408 is an orally active dual DGK α/ζ inhibitor that restores T cell-mediated anti-tumor immunity by enhancing T cell signaling [1] .
- GC79592(S)-DSM1465CAS: 3109381-05-4Purity: >99.50%
(S)-DSM1465 is a Plasmodium dihydroorotate dehydrogenase ( DHODH ) inhibitor.
- GC79593DPP-4-IN-18CAS: 486460-31-5Purity: >98.00%
DPP-4-IN-18 (Sitagliptin impurity 3) (Compound 4) impurity 3 is a potent, selective and orally active DPP-4 inhibitor with an IC 50 of 27 nM.
- GC795941-(4-Methoxyphenyl)-1-propanolCAS: 5349-60-0Purity: >99.00%
1-(4-Methoxyphenyl)-1-propanol (Compound 2) is an orally active derivative of anethole.
- GC79595N-NitrosoglyphosateCAS: 56516-72-4Purity: >98.00%
N-Nitrosoglyphosate is the nitrosamine degradation product of glyphosate herbicidee.
- GC79596(S)-4-HydroxymephenytoinCAS: 82695-93-0Purity: >98.00%
(S) -4-Hydroxy mephenytoin is a metabolite derived from the stereoselective metabolism of mephenytoin.
- GC79597N-Acetyl-S-(N-methylcarbamoyl)cysteineCAS: 103974-29-4Purity: >98.00%
N-Acetyl-S-(N-methylcarbamoyl) cysteine is a metabolite of solvent N,N-dimethylformamide and could be used for monitoring industrial exposure.
- GC79598Tyramine O-sulfate sodiumCAS: 2083619-07-0Purity: >99.00%
Tyramine O-sulfate (Tyramine sulfate) sodium is a metabolite of Tyramine formed via sulfation, which serves as a biomarker for depression.
- GC79599Melatonin-OHCAS: 67199-08-0Purity: >98.50%
Melatonin -OH is an oxidative Melatonin metabolite with free radical-scavenging activity.
- GC796003-Hydroxybenzo[a]pyreneCAS: 13345-21-6Purity: >98.00%
3-Hydroxybenzo[a]pyrene (3-OHBaP) is a preferable biomarker to assess exposure to benzo[a]pyrene (BaP), a carcinogenic agent.
- GC796025Oxo-MEHTPCAS: 1684398-40-0Purity: >98.00%
5Oxo-MEHTP is an urinary metabolite of di(2-ethylhexyl) terephthalate (DEHTP).
- GC796033-(3-Sulfooxyphenyl)propanoic acid disodiumPurity: >98.00%
3-(3-Sulfooxyphenyl) propanoic acid disodium is a metabolite of Echinacoside.
- GC79604Fenthion sulfoxideCAS: 3761-41-9Purity: >98.00%
Fenthion sulfoxide is a metabolite of the organophosphate insecticide Fenthion.
- GC796051-(7-Hydroxy-4-methyloctyl) 1,2-cyclohexanedicarboxylateCAS: 1637562-52-7Purity: >98.00%
1-(7-Hydroxy-4-methyloctyl) 1,2-cyclohexanedicarboxylate is a metabolite of di (isononyl) cyclohexane-1,2-dicarboxylate (DINCH), an alternative for phthalate plasticizers.
- GC7960620α-DihydrodydrogesteroneCAS: 4243-74-7Purity: >98.00%
20α-dihydrodydrogesterone is the major active metabolite of Dydrogesterone produced in the human body after oral administration.
- GC79607Tiopronin disulfideCAS: 21269-37-4Purity: >98.00%
Tiopronin disulfide, a Tiopronin dimer, is an oxidative product of Tiopronin.
- GC796081,2-Cyclohexanedicarboxylic acid mono 4-methyl-7-carboxy-heptyl esterCAS: 1637562-51-6Purity: >98.00%
1,2-Cyclohexanedicarboxylic Acid Mono 4-Methyl-7-carboxy-heptyl Ester is a secondary oxidized metabolite of di(isononyl) cyclohexane-1,2-dicarboxylate (DINCH), an alternative for phthalate plasticizer.
- GC796092-Hydroxymethyl olanzapineCAS: 174756-45-7Purity: >98.00%
2-Hydroxymethyl olanzapine is a metabolite and a degradation product of Olanzapine [1] [2] .
- GC796107-Hydroxycoumarin glucuronideCAS: 66695-14-5Purity: >98.00%
7-Hydroxycoumarin glucuronide is a transport substrate and main human coumarin metabolite.
- GC79611Bupivacaine N-oxide hydrochlorideCAS: 1796927-05-3Purity: >98.00%
Bupivacaine N-oxide hydrochloride is a metabolite of Bupivacaine.
- GC796131',4-Dihydroxy midazolamCAS: 64740-68-7Purity: >98.00%
1',4-Dihydroxymidazolam is a hydroxylated metabolite produced by cytochrome P450 -mediated metabolism of midazolam in the liver [1] .
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC79590 | (Rac)-δ-Viniferin | - | >98.50% | |
(Rac)-δ-Viniferin is a racemate of δ-Viniferin, an isomer of ε-Viniferin. | ||||
| GC79591 | (1R)-BMS-986408 | 2618418-11-2 | >99.00% | |
(1R)-BMS-986408 is an orally active dual DGK α/ζ inhibitor that restores T cell-mediated anti-tumor immunity by enhancing T cell signaling [1] . | ||||
| GC79592 | (S)-DSM1465 | 3109381-05-4 | >99.50% | |
(S)-DSM1465 is a Plasmodium dihydroorotate dehydrogenase ( DHODH ) inhibitor. | ||||
| GC79593 | DPP-4-IN-18 | 486460-31-5 | >98.00% | |
DPP-4-IN-18 (Sitagliptin impurity 3) (Compound 4) impurity 3 is a potent, selective and orally active DPP-4 inhibitor with an IC 50 of 27 nM. | ||||
| GC79594 | 1-(4-Methoxyphenyl)-1-propanol | 5349-60-0 | >99.00% | |
1-(4-Methoxyphenyl)-1-propanol (Compound 2) is an orally active derivative of anethole. | ||||
| GC79595 | N-Nitrosoglyphosate | 56516-72-4 | >98.00% | |
N-Nitrosoglyphosate is the nitrosamine degradation product of glyphosate herbicidee. | ||||
| GC79596 | (S)-4-Hydroxymephenytoin | 82695-93-0 | >98.00% | |
(S) -4-Hydroxy mephenytoin is a metabolite derived from the stereoselective metabolism of mephenytoin. | ||||
| GC79597 | N-Acetyl-S-(N-methylcarbamoyl)cysteine | 103974-29-4 | >98.00% | |
N-Acetyl-S-(N-methylcarbamoyl) cysteine is a metabolite of solvent N,N-dimethylformamide and could be used for monitoring industrial exposure. | ||||
| GC79598 | Tyramine O-sulfate sodium | 2083619-07-0 | >99.00% | |
Tyramine O-sulfate (Tyramine sulfate) sodium is a metabolite of Tyramine formed via sulfation, which serves as a biomarker for depression. | ||||
| GC79599 | Melatonin-OH | 67199-08-0 | >98.50% | |
Melatonin -OH is an oxidative Melatonin metabolite with free radical-scavenging activity. | ||||
| GC79600 | 3-Hydroxybenzo[a]pyrene | 13345-21-6 | >98.00% | |
3-Hydroxybenzo[a]pyrene (3-OHBaP) is a preferable biomarker to assess exposure to benzo[a]pyrene (BaP), a carcinogenic agent. | ||||
| GC79601 | Diazoxon | 962-58-3 | >98.00% | |
Diazoxon is a metabolite of Diazinon. | ||||
| GC79602 | 5Oxo-MEHTP | 1684398-40-0 | >98.00% | |
5Oxo-MEHTP is an urinary metabolite of di(2-ethylhexyl) terephthalate (DEHTP). | ||||
| GC79603 | 3-(3-Sulfooxyphenyl)propanoic acid disodium | - | >98.00% | |
3-(3-Sulfooxyphenyl) propanoic acid disodium is a metabolite of Echinacoside. | ||||
| GC79604 | Fenthion sulfoxide | 3761-41-9 | >98.00% | |
Fenthion sulfoxide is a metabolite of the organophosphate insecticide Fenthion. | ||||
| GC79605 | 1-(7-Hydroxy-4-methyloctyl) 1,2-cyclohexanedicarboxylate | 1637562-52-7 | >98.00% | |
1-(7-Hydroxy-4-methyloctyl) 1,2-cyclohexanedicarboxylate is a metabolite of di (isononyl) cyclohexane-1,2-dicarboxylate (DINCH), an alternative for phthalate plasticizers. | ||||
| GC79606 | 20α-Dihydrodydrogesterone | 4243-74-7 | >98.00% | |
20α-dihydrodydrogesterone is the major active metabolite of Dydrogesterone produced in the human body after oral administration. | ||||
| GC79607 | Tiopronin disulfide | 21269-37-4 | >98.00% | |
Tiopronin disulfide, a Tiopronin dimer, is an oxidative product of Tiopronin. | ||||
| GC79608 | 1,2-Cyclohexanedicarboxylic acid mono 4-methyl-7-carboxy-heptyl ester | 1637562-51-6 | >98.00% | |
1,2-Cyclohexanedicarboxylic Acid Mono 4-Methyl-7-carboxy-heptyl Ester is a secondary oxidized metabolite of di(isononyl) cyclohexane-1,2-dicarboxylate (DINCH), an alternative for phthalate plasticizer. | ||||
| GC79609 | 2-Hydroxymethyl olanzapine | 174756-45-7 | >98.00% | |
2-Hydroxymethyl olanzapine is a metabolite and a degradation product of Olanzapine [1] [2] . | ||||
| GC79610 | 7-Hydroxycoumarin glucuronide | 66695-14-5 | >98.00% | |
7-Hydroxycoumarin glucuronide is a transport substrate and main human coumarin metabolite. | ||||
| GC79611 | Bupivacaine N-oxide hydrochloride | 1796927-05-3 | >98.00% | |
Bupivacaine N-oxide hydrochloride is a metabolite of Bupivacaine. | ||||
| GC79612 | BTS44596 | 139542-32-8 | >98.00% | |
BTS44596 (Prochloraz-desimidazole-formylamino) is a metabolite of the antifungal agent Prochloraz. | ||||
| GC79613 | 1',4-Dihydroxy midazolam | 64740-68-7 | >98.00% | |
1',4-Dihydroxymidazolam is a hydroxylated metabolite produced by cytochrome P450 -mediated metabolism of midazolam in the liver [1] . | ||||