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Signaling Pathways

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.

Targets for  Signaling Pathways

Products for  Signaling Pathways

  1. Cat.No. Product Name Information
  2. GC19789 Hyaluronidase

     Hyaluronidase;>300u/mg

     Hyaluronidase  Chemical Structure
  3. GC19566 N-Nitrosodiethylamine  N-Nitrosodiethylamine  Chemical Structure
  4. GC50569 NLRP3-IN-2

    NLRP3 inflammasome inhibitor

     NLRP3-IN-2  Chemical Structure
  5. GC63267 α-​Chaconine  α-​Chaconine  Chemical Structure
  6. GC45195 α,β-Methyleneadenosine 5'-triphosphate (sodium salt)

    α,β-Methyleneadenosine 5'-triphosphate (αβ-methylene ATP) is a phosphonic analog of ATP that is characterized by the replacement of the bridging oxygen atom between the α- and β-phosphate groups with methylene.

    α,β-Methyleneadenosine 5'-triphosphate (sodium salt)  Chemical Structure
  7. GC45194 α-(difluoromethyl)-DL-Arginine

    Bacteria synthesize the cellular growth factor putrescine through a number of pathways.

    α-(difluoromethyl)-DL-Arginine  Chemical Structure
  8. GC63268 α-Amyrin palmitate α-Amyrin palmitate  Chemical Structure
  9. GC41183 α-Carotene

    α-Carotene is a precursor of vitamin A that has been found in various fruits and vegetables.

    α-Carotene  Chemical Structure
  10. GC63269 α-Conotoxin PIA TFA α-Conotoxin PIA TFA  Chemical Structure
  11. GC63723 α-Conotoxin PnIA TFA α-Conotoxin PnIA TFA  Chemical Structure
  12. GC39464 α-Cyclodextrin α-Cyclodextrin  Chemical Structure
  13. GC40702 α-D-Galactopyranosylphenyl isothiocyanate

    α-D-Galactopyranosylphenyl isothiocyanate is a chemically activated form of galactose that has been used to prepare various neoglycoproteins, which consist of a glycosylated serum albumin substituted with either fluorescein or methotrexate.

    α-D-Galactopyranosylphenyl isothiocyanate  Chemical Structure
  14. GC45204 α-Ecdysone

    α-Ecdysone is a prohormone of 20-hydroxy ecdysone, an insect-molting, ecdysteroid hormone.

    α-Ecdysone  Chemical Structure
  15. GC38042 α-Factor Mating Pheromone, yeast (TFA) α-Factor Mating Pheromone, yeast (TFA)  Chemical Structure
  16. GC45206 α-GalCer analog 8

    α-Galactosylceramide analog 8 (α-GalCer analog 8) is a triazole derivative of α-galactosylceramide.

    α-GalCer analog 8  Chemical Structure
  17. GC45207 α-hydroxy Farnesyl Phosphonic Acid α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). α-hydroxy Farnesyl Phosphonic Acid  Chemical Structure
  18. GC45208 α-hydroxy Metoprolol α-hydroxy Metoprolol is an active metabolite of the β1-adrenergic receptor blocker metoprolol. α-hydroxy Metoprolol  Chemical Structure
  19. GC45210 α-Linolenic Acid (sodium salt) α-Linolenic acid (ALA) is an essential fatty acid found in leafy green vegetables. α-Linolenic Acid (sodium salt)  Chemical Structure
  20. GC45601 α-Linolenic Acid ethyl ester-d5   α-Linolenic Acid ethyl ester-d5  Chemical Structure
  21. GC45602 α-Linolenic Acid-d5 MaxSpec• Standard   α-Linolenic Acid-d5 MaxSpec• Standard  Chemical Structure
  22. GC63749 α-Lipoic Acid-d5 α-Lipoic Acid-d5  Chemical Structure
  23. GC40718 α-Muricholic Acid

    α-Muricholic acid is a murine-specific primary bile acid.

    α-Muricholic Acid  Chemical Structure
  24. GC45213 α-NETA Choline acetyltransferase (ChAT) mediates the synthesis of the neurotransmitter acetylcholine from acetyl-CoA and choline. α-NETA  Chemical Structure
  25. GC41499 α-Phellandrene α-Phellandrene is a cyclic monoterpene that has been found in various plants, including Cannabis, and has diverse biological activities. α-Phellandrene  Chemical Structure
  26. GC40480 α-Phenyl-α-(2-pyridyl)acetonitrile α-Phenyl-α-(2-pyridyl)thioacetamide, also known as antigastrin and SC-15396, is an inhibitor of gastric acid secretion. α-Phenyl-α-(2-pyridyl)acetonitrile  Chemical Structure
  27. GC38287 α-Pyridone α-Pyridone  Chemical Structure
  28. GC63941 α-Solanine α-Solanine  Chemical Structure
  29. GC41501 α-Terpinene α-Terpinene is a terpenoid that has been found in Cannabis and has diverse biological activities, including acaricidal, antiprotozoal, and antioxidant properties. α-Terpinene  Chemical Structure
  30. GC63615 α-Thujone α-Thujone  Chemical Structure
  31. GC37980 α-Tocopherol phosphate α-Tocopherol phosphate  Chemical Structure
  32. GC45224 α-Truxillic Acid

    α-Truxillic acid can be formed by the dimerization of two molecules of α-trans-cinnamic acid.

    α-Truxillic Acid  Chemical Structure
  33. GC40753 α-Zearalanol α-Zearalanol is an active metabolite formed by reduction of α-zearalenol, an estrogen receptor antagonist. α-Zearalanol  Chemical Structure
  34. GC38873 α2β1 Integrin Ligand Peptide TFA α2β1 Integrin Ligand Peptide TFA  Chemical Structure
  35. GC62380 αvβ1 integrin-IN-1 αvβ1 integrin-IN-1  Chemical Structure
  36. GC62566 αvβ1 integrin-IN-1 TFA αvβ1 integrin-IN-1 TFA  Chemical Structure
  37. GC49467 β-Aescin A triterpenoid saponin with diverse biological activities β-Aescin  Chemical Structure
  38. GC63273 β-Amyloid (1-14),mouse,rat β-Amyloid (1-14),mouse,rat  Chemical Structure
  39. GC63274 β-Amyloid (1-42), (rat/mouse) (TFA) β-Amyloid (1-42), (rat/mouse) (TFA)  Chemical Structure
  40. GC37984 β-Amyloid (1-42), rat β-Amyloid (1-42), rat  Chemical Structure
  41. GC61394 β-Amyloid (1-42), rat TFA β-Amyloid (1-42), rat TFA  Chemical Structure
  42. GC37991 β-Amyloid 15-21 β-Amyloid 15-21  Chemical Structure
  43. GC45603 β-Amyrin   β-Amyrin  Chemical Structure
  44. GC45225 β-Apooxytetracycline β-Apooxytetracycline is a potential impurity found in commercial preparations of oxytetracycline. β-Apooxytetracycline  Chemical Structure
  45. GC60391 β-Casomorphin, bovine TFA β-Casomorphin, bovine TFA  Chemical Structure
  46. GC61484 β-Casomorphin, human TFA β-Casomorphin, human TFA  Chemical Structure
  47. GC62432 β-catenin-IN-2 β-catenin-IN-2  Chemical Structure
  48. GC40789 β-Cembrenediol β-Cembrenediol (β-CBT) is a natural product from tobacco plants that is found in cigarette smoke condensate. β-Cembrenediol  Chemical Structure
  49. GC63275 β-Cryptoxanthin β-Cryptoxanthin  Chemical Structure
  50. GC41267 β-cyano-L-Alanine

    Hydrogen sulfide (H2S) is a naturally-occurring gasotransmitter with vasodilator and inflammatory modulating activity.

    β-cyano-L-Alanine  Chemical Structure
  51. GC63276 β-Cyclocitral β-Cyclocitral  Chemical Structure
  52. GC45228 β-Cyclodextrin β-Cyclodextrin (β-CD) is a cyclic oligosaccharide that contains seven D-(+)-glucopyranose units and has been used to improve the aqueous solubility of various compounds, especially those containing a phenyl group. β-Cyclodextrin  Chemical Structure
  53. GC63277 β-Cyclogeraniol β-Cyclogeraniol  Chemical Structure
  54. GC45232 β-D-Glucosamine Pentaacetate β-D-Glucosamine pentaacetate is an N-acetylglucosamine derivative that has been shown to promote hyaluronic acid production. β-D-Glucosamine Pentaacetate  Chemical Structure
  55. GC40777 β-D-Glucose

    D-Glucose, a naturally occurring monosaccharide found in plants, is the primary energy source for living organisms.

    β-D-Glucose  Chemical Structure
  56. GC63278 β-D-Glucose pentaacetate β-D-Glucose pentaacetate  Chemical Structure
  57. GC45230 β-Defensin-3 (human) (trifluoroacetate salt) β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. β-Defensin-3 (human) (trifluoroacetate salt)  Chemical Structure
  58. GC45231 β-Defensin-4 (human) (trifluoroacetate salt) β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. β-Defensin-4 (human) (trifluoroacetate salt)  Chemical Structure
  59. GC41623 β-Elemonic Acid β-Elemonic acid is a triterpene isolated from Boswellia (Burseraceae) that exhibits anticancer activity. β-Elemonic Acid  Chemical Structure
  60. GC45234 β-Endorphin (1-27) (human) (trifluoroacetate salt) β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). β-Endorphin (1-27) (human) (trifluoroacetate salt)  Chemical Structure
  61. GA24007 β-Endorphin (30-31) (bovine, camel, mouse, ovine) The dipeptide Gly-Gln, which is naturally derived from the posttranslational processing of β-endorphin, exhibited an inhibitory action on cell firing when applied iontophoretically to brainstem neurons in the rat. Moreover, it seems to be a neurotrophic regulator of acetylcholinesterase in the mammalian sympathetic ganglion. Gly-Gln suppressed morphine withdrawal symptoms in rats. Gly-Gln has found use as a Gln source in parenteral nutrition, see also G-1210. β-Endorphin (30-31) (bovine, camel, mouse, ovine)  Chemical Structure
  62. GC45236 β-Endorphin (rat) β-Endorphin (β-EP) is an endogenous opioid neuropeptide with diverse biological activities. β-Endorphin (rat)  Chemical Structure
  63. GC38030 β-Endorphin, equine (TFA) β-Endorphin, equine (TFA)  Chemical Structure
  64. GC62551 β-Hydroxypropiovanillone β-Hydroxypropiovanillone  Chemical Structure
  65. GC49647 β-Hyodeoxycholic Acid (hydrate) A 3β epimer of hyodeoxycholic acid β-Hyodeoxycholic Acid (hydrate)  Chemical Structure
  66. GC62235 β-Lactamase-IN-2 β-Lactamase-IN-2  Chemical Structure
  67. GC38007 β-Melanocyte Stimulating Hormone (MSH), human TFA β-Melanocyte Stimulating Hormone (MSH), human TFA  Chemical Structure
  68. GC40719 β-Muricholic Acid A murine-specific primary bile acid β-Muricholic Acid  Chemical Structure
  69. GC41502 β-Myrcene β-Myrcene is a terpene that has been found in Cannabis and has antioxidative properties. β-Myrcene  Chemical Structure
  70. GC45604 β-Rubromycin   β-Rubromycin  Chemical Structure
  71. GC38008 β-Zearalenol β-Zearalenol  Chemical Structure
  72. GC61462 γ-1-Melanocyte Stimulating Hormone (MSH), amide γ-1-Melanocyte Stimulating Hormone (MSH), amide  Chemical Structure
  73. GC38010 γ-Aminobutyric acid γ-Aminobutyric acid  Chemical Structure
  74. GC40551 γ-CEHC The major tocopherol obtained from natural dietary sources is γ-tocopherol, whereas α-tocopherol is the form of Vitamin E typically obtained from synthetic supplements. γ-CEHC  Chemical Structure
  75. GC63279 γ-Glu-Gly TFA γ-Glu-Gly TFA  Chemical Structure
  76. GC63280 γ-Hexalactone γ-Hexalactone  Chemical Structure
  77. GC40790 γ-Linolenic Acid ethyl ester γ-Linolenic acid (GLA) is an ω-6 fatty acid which can be elongated to arachidonic acid for endogenous eicosanoid synthesis. γ-Linolenic Acid ethyl ester  Chemical Structure
  78. GC41503 γ-Terpinene γ-Terpinene is a monoterpene that has been found in various plants, including C. γ-Terpinene  Chemical Structure
  79. GC41109 δ12-Prostaglandin J2 δ12-PGJ2 is a decomposition product of PGD2 in aqueous media in the presence of albumin. δ12-Prostaglandin J2  Chemical Structure
  80. GC45238 δ14-Triamcinolone acetonide δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. δ14-Triamcinolone acetonide  Chemical Structure
  81. GC45239 δ4-Abiraterone δ4-Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone. δ4-Abiraterone  Chemical Structure
  82. GC62708 σ1 Receptor antagonist-1 σ1 Receptor antagonist-1  Chemical Structure
  83. GC41552 ω-3 Arachidonic Acid ω-3 Arachidonic acid is a rare PUFA found in trace amounts in dietary sources. ω-3 Arachidonic Acid  Chemical Structure
  84. GC41393 ω-3 Arachidonic Acid methyl ester ω-3 Fatty acids, represented primarily by docosahexaenoic acid, eicosapentaenoic acid, and α-linoleate, are essential dietary nutrients required for normal growth and development. ω-3 Arachidonic Acid methyl ester  Chemical Structure
  85. GC62067 ω-Conotoxin GVIA TFA ω-Conotoxin GVIA TFA  Chemical Structure
  86. GA24016 ω-Conotoxin MVIIA ω-Conotoxin MVIIA, originally isolated from the venom of the fish-hunting cone snail Conus magus, is a blocker of voltage-sensitive Ca²? channels in neurons. The peptide has been used to identify different Ca²? channel subtypes in amphibian brain. ω-Conotoxin MVIIA  Chemical Structure
  87. GC63281 ω-Pentadecalactone ω-Pentadecalactone  Chemical Structure
  88. GC62478 Ζ-Stat-2 Ζ-Stat-2  Chemical Structure
  89. GC45713 (±)-α-Tocopherol Acetate (±)-α-Tocopherol Acetate  Chemical Structure
  90. GC38194 (±)-10-Hydroxycamptothecin (±)-10-Hydroxycamptothecin  Chemical Structure
  91. GC41657 (±)-2-Amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (hydrobromide) (±)-2-Amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (6,7-ADTN) is a dopamine receptor agonist (EC50s = 3.5 and 0.65 μM in rat striatal and nucleus accumbens homogenates, respectively). (±)-2-Amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (hydrobromide)  Chemical Structure
  92. GC41658 (±)-2-hydroxy Ibuprofen (±)-2-hydroxy Ibuprofen is a metabolite of ibuprofen . (±)-2-hydroxy Ibuprofen  Chemical Structure
  93. GC41661 (±)-4-hydroxy Propranolol β-D-Glucuronide (±)-4-hydroxy Propranolol β-D-glucuronide is a metabolite of (±)-4-hydroxy propranolol, which is a metabolite of propranolol. (±)-4-hydroxy Propranolol β-D-Glucuronide  Chemical Structure
  94. GC40559 (±)-Alliin Alliin is a cysteine sulfoxide constituent of garlic that is converted by alliinase to allicin, which imparts its pungent aroma and flavor. (±)-Alliin  Chemical Structure
  95. GC62726 (±)-Amiflamine (±)-Amiflamine  Chemical Structure
  96. GC34961 (±)-BI-D (±)-BI-D  Chemical Structure
  97. GC41668 (±)-Clopidogrel (hydrochloride) Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). (±)-Clopidogrel (hydrochloride)  Chemical Structure
  98. GC60394 (±)-Duloxetine hydrochloride (±)-Duloxetine hydrochloride  Chemical Structure
  99. GC41669 (±)-Enterolactone Diets high in fiber contain plant lignan species that may be directly responsible for some observed health benefits of these diets. (±)-Enterolactone  Chemical Structure
  100. GC41670 (±)-Epinephrine (hydrochloride) (±)-Epinephrine is a natural neurotransmitter that is released from the adrenal medulla and activates adrenoceptors (Kis = 15, 735, and 3,970 nM for α1A-, β2-, and β1-adrenergic receptors, respectively). (±)-Epinephrine (hydrochloride)  Chemical Structure
  101. GC41671 (±)-Equol 4'-sulfate (sodium salt)

    (±)-Equol 4'-sulfate is a gut-mediated phase II metabolite of the isoflavonoid phytoestrogen (±)-equol.

    (±)-Equol 4'-sulfate (sodium salt)  Chemical Structure

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