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(39631)
- GC81385PA22-2 TFAPurity: >95.50%
PA22-2 (IKVAV sequence; Laminin A-chain fragment) TFA is a laminin receptor ligand.
- GC81386Noratherosperminine hydrochlorideCAS: 2760889-73-2Purity: >99.50%
Noratherosperminine hydrochloride is a phenanthrene alkaloid found in the stem bark of Cryptocarya nigra [1] .
- GC813871-Methyl-N-(4-(piperidin-1-yl)phenyl)-1H-imidazole-4-sulfonamideCAS: 708988-50-5Purity: >98.00%
1-Methyl-N-(4-(piperidin-1-yl)phenyl)-1H-imidazole-4-sulfonamide is a pharmaceutical synthesis intermediate.
- GC81388AmisometradineCAS: 550-28-7Purity: >98.00%
Amisometradine is an orally active aminouracil diuretic with a diuretic potency approximately 40% that of Mersalyl (when administered intramuscularly).
- GC81389Lyciumin CCAS: 150394-23-3Purity: >98.00%
Lyciumin C is a monocyclic octapeptide containing a novel C-N linkage between tryptophan N1 and glycine Cα, and can be found in the root bark of Lycium chinense MILL [1] .
- GC81390p-SCN-MacropaCAS: 2417821-30-6Purity: >96.00%
p-SCN-Macropa is a bifunctional macrocyclic chelator featuring macrocyclic polyamine skeletons and thiocyanate (-SCN) reactive moieties.
- GC81391Dipotassium phosphiteCAS: 13492-26-7Purity: >95.00%
Dipotassium phosphite is a phosphite salt and is an antibacterial agent.
- GC813928-Oxo-dGTP trisodium solution (100 mM)Purity: >98.50%
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E.
- GC81394PPA-037 TFAPurity: >99.00%
PPA-037 TFA is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 ( CDK12 ).
- GC81395ddhCTP trisodium solution (100 mM ± 3 mM)Purity: >98.00%
ddhCTP trisodium solution (100 mM ± 3 mM) is an endogenously produced pyrimidine base analog with a K d of 17.0 nM for LLDH and an IC 50 of 55.8 μM for GAPDH.
- GC81396ARCA triammonium solution (100 mM)Purity: >98.00%
ARCA (triammonium) solution (100 mM) (Anti-Reverse cap analog triammonium solution (100 mM); m 2 7,3'O Gppp triammonium solution (100 mM)) is a 5′-cap analog.
- GC813977-Methyl-diguanosine triphosphate ammonium solution (100 mM)CAS: 75252-12-9Purity: >98.50%
7-Methyl-diguanosine triphosphate (m7Gp3G) ammonium is an mRNA cap structure analog that inhibits in vitro protein synthesis by binding to the translation initiation complex.
- GC81398m7(3'OMeG)(5')ppp(5')m6(2'OMeA)pG tetraammonium solution (100 mM)Purity: >99.00%
m7(3'OMeG)(5')ppp(5')m6(2'OMeA)pG tetraammonium solution (100 mM) is a cap analog that can be used for in vitro transcription of mRNA.
- GC81399m7(3'AcmG)(5')ppp(5')(2'OMeA)pG trisodium solution (100 mM)Purity: >98.50%
m7(3'AcmG)(5')ppp(5')(2'OMeA)pG trisodium, a cap analogue derived from patent WO2023159930A1, can be used for the synthesis of mRNA [1] .
- GC81400Adenosine-3',5'-bisphosphate ammonium solution (100 mM)Purity: >99.00%
Adenosine-3',5'-bisphosphate ammonium is a XRN1 inhibitor ( IC 50 = 36 nM).
- GC81402Sp-ATPαS tetrasodium solution (100mM)Purity: >98.50%
Sp-ATPαS tetrasodium is a thiophosphonate analogue of ATP.
- GC81403Allyl thiosulfateCAS: 6363-01-5Purity: >99.50%
Allyl thiosulfate (Sodium 2-propenyl thiosulfate) is found in Allium plants such as garlic and onion.
- GC81404Citramalic acidCAS: 597-44-4Purity: >99.00%
Citramalic acid is an organic acid and soil phosphorus-solubilizing agent.
- GC814054-Amino-3-hydroxyphenylalanine dihydrochloridePurity: >98.50%
4-Amino-3-hydroxyphenylalanine dihydrochloride is a photodegradation product of Eumelanin.
- GC81406Magnesium L-glutamate tetrahydratePurity: >99.50%
Magnesium L-glutamate tetrahydrate is a cysteine derivative.
- GC81407(S)-5-Acetamido-2-aminopentanoic acidCAS: 2185-16-2Purity: >97.00%
(S)-5-Acetamido-2-aminopentanoic acid is an adamantane-labeled glutamine analog [1] .
- GC81408Phosphotungstic Acid Negative Staining Solution (3%, pH 7.0)Purity: >98.00%
Phosphotungstic Acid Negative Staining Solution (3%, pH 7.0) is an electron microscopy negative stain.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81385 | PA22-2 TFA | - | >95.50% | |
PA22-2 (IKVAV sequence; Laminin A-chain fragment) TFA is a laminin receptor ligand. | ||||
| GC81386 | Noratherosperminine hydrochloride | 2760889-73-2 | >99.50% | |
Noratherosperminine hydrochloride is a phenanthrene alkaloid found in the stem bark of Cryptocarya nigra [1] . | ||||
| GC81387 | 1-Methyl-N-(4-(piperidin-1-yl)phenyl)-1H-imidazole-4-sulfonamide | 708988-50-5 | >98.00% | |
1-Methyl-N-(4-(piperidin-1-yl)phenyl)-1H-imidazole-4-sulfonamide is a pharmaceutical synthesis intermediate. | ||||
| GC81388 | Amisometradine | 550-28-7 | >98.00% | |
Amisometradine is an orally active aminouracil diuretic with a diuretic potency approximately 40% that of Mersalyl (when administered intramuscularly). | ||||
| GC81389 | Lyciumin C | 150394-23-3 | >98.00% | |
Lyciumin C is a monocyclic octapeptide containing a novel C-N linkage between tryptophan N1 and glycine Cα, and can be found in the root bark of Lycium chinense MILL [1] . | ||||
| GC81390 | p-SCN-Macropa | 2417821-30-6 | >96.00% | |
p-SCN-Macropa is a bifunctional macrocyclic chelator featuring macrocyclic polyamine skeletons and thiocyanate (-SCN) reactive moieties. | ||||
| GC81391 | Dipotassium phosphite | 13492-26-7 | >95.00% | |
Dipotassium phosphite is a phosphite salt and is an antibacterial agent. | ||||
| GC81392 | 8-Oxo-dGTP trisodium solution (100 mM) | - | >98.50% | |
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. | ||||
| GC81393 | KP-1212 | 114522-16-6 | >99.00% | |
KP-1212 is a nucleoside. | ||||
| GC81394 | PPA-037 TFA | - | >99.00% | |
PPA-037 TFA is an orally active, highly potent and selective inhibitor of cyclin-dependent kinase 12 ( CDK12 ). | ||||
| GC81395 | ddhCTP trisodium solution (100 mM ± 3 mM) | - | >98.00% | |
ddhCTP trisodium solution (100 mM ± 3 mM) is an endogenously produced pyrimidine base analog with a K d of 17.0 nM for LLDH and an IC 50 of 55.8 μM for GAPDH. | ||||
| GC81396 | ARCA triammonium solution (100 mM) | - | >98.00% | |
ARCA (triammonium) solution (100 mM) (Anti-Reverse cap analog triammonium solution (100 mM); m 2 7,3'O Gppp triammonium solution (100 mM)) is a 5′-cap analog. | ||||
| GC81397 | 7-Methyl-diguanosine triphosphate ammonium solution (100 mM) | 75252-12-9 | >98.50% | |
7-Methyl-diguanosine triphosphate (m7Gp3G) ammonium is an mRNA cap structure analog that inhibits in vitro protein synthesis by binding to the translation initiation complex. | ||||
| GC81398 | m7(3'OMeG)(5')ppp(5')m6(2'OMeA)pG tetraammonium solution (100 mM) | - | >99.00% | |
m7(3'OMeG)(5')ppp(5')m6(2'OMeA)pG tetraammonium solution (100 mM) is a cap analog that can be used for in vitro transcription of mRNA. | ||||
| GC81399 | m7(3'AcmG)(5')ppp(5')(2'OMeA)pG trisodium solution (100 mM) | - | >98.50% | |
m7(3'AcmG)(5')ppp(5')(2'OMeA)pG trisodium, a cap analogue derived from patent WO2023159930A1, can be used for the synthesis of mRNA [1] . | ||||
| GC81400 | Adenosine-3',5'-bisphosphate ammonium solution (100 mM) | - | >99.00% | |
Adenosine-3',5'-bisphosphate ammonium is a XRN1 inhibitor ( IC 50 = 36 nM). | ||||
| GC81401 | DD04107 | 1202877-06-2 | >99.50% | |
DD04107 is a neuronal exocytosis inhibitor with a rat Syt1-C2B domain binding K d of 2.4 μM. | ||||
| GC81402 | Sp-ATPαS tetrasodium solution (100mM) | - | >98.50% | |
Sp-ATPαS tetrasodium is a thiophosphonate analogue of ATP. | ||||
| GC81403 | Allyl thiosulfate | 6363-01-5 | >99.50% | |
Allyl thiosulfate (Sodium 2-propenyl thiosulfate) is found in Allium plants such as garlic and onion. | ||||
| GC81404 | Citramalic acid | 597-44-4 | >99.00% | |
Citramalic acid is an organic acid and soil phosphorus-solubilizing agent. | ||||
| GC81405 | 4-Amino-3-hydroxyphenylalanine dihydrochloride | - | >98.50% | |
4-Amino-3-hydroxyphenylalanine dihydrochloride is a photodegradation product of Eumelanin. | ||||
| GC81406 | Magnesium L-glutamate tetrahydrate | - | >99.50% | |
Magnesium L-glutamate tetrahydrate is a cysteine derivative. | ||||
| GC81407 | (S)-5-Acetamido-2-aminopentanoic acid | 2185-16-2 | >97.00% | |
(S)-5-Acetamido-2-aminopentanoic acid is an adamantane-labeled glutamine analog [1] . | ||||
| GC81408 | Phosphotungstic Acid Negative Staining Solution (3%, pH 7.0) | - | >98.00% | |
Phosphotungstic Acid Negative Staining Solution (3%, pH 7.0) is an electron microscopy negative stain. | ||||
