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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.

Products for  Signaling Pathways

  1. Cat.No. Product Name Information
  2. GC68479 MMRi62 MMRi62  Chemical Structure
  3. GC68478 Bictegravir sodium Bictegravir sodium  Chemical Structure
  4. GC68477 Stepronin Stepronin  Chemical Structure
  5. GC68476 (S)-Nicardipine (S)-Nicardipine  Chemical Structure
  6. GC68475 (R)-Nicardipine (R)-Nicardipine  Chemical Structure
  7. GC68474 Pivanex Pivanex  Chemical Structure
  8. GC68473 Methyl carnosate Methyl carnosate  Chemical Structure
  9. GC68471 Nifurpirinol Nifurpirinol  Chemical Structure
  10. GC68470 SPD304 dihydrochloride SPD304 dihydrochloride  Chemical Structure
  11. GC68469 CID1231538 CID1231538  Chemical Structure
  12. GC68468 MPO-IN-3 MPO-IN-3  Chemical Structure
  13. GC68465 SDH-IN-1 SDH-IN-1  Chemical Structure
  14. GC68464 ALDH1A3-IN-1 ALDH1A3-IN-1  Chemical Structure
  15. GC68463 ULK1-IN-2 ULK1-IN-2  Chemical Structure
  16. GC68462 ALDH1A3-IN-2 ALDH1A3-IN-2  Chemical Structure
  17. GC68461 TrxR-IN-5 TrxR-IN-5  Chemical Structure
  18. GC68460 PDE4B-IN-3 PDE4B-IN-3  Chemical Structure
  19. GC68459 NHS-SS-Ac NHS-SS-Ac  Chemical Structure
  20. GC68458 HS-243 HS-243  Chemical Structure
  21. GC68457 Mab Aspartate Decarboxylase-IN-1 Mab Aspartate Decarboxylase-IN-1  Chemical Structure
  22. GC68455 CP681301 CP681301  Chemical Structure
  23. GC68453 ITMN 4077 ITMN 4077  Chemical Structure
  24. GC68452 2,4,6-Triiodophenol 2,4,6-Triiodophenol  Chemical Structure
  25. GC68451 SRI-37330 SRI-37330  Chemical Structure
  26. GC68450 Hsp90-IN-17 hydrochloride Hsp90-IN-17 hydrochloride  Chemical Structure
  27. GC68449 CA inhibitor 1 CA inhibitor 1  Chemical Structure
  28. GC68448 AOH1160 AOH1160  Chemical Structure
  29. GC68447 GSK143 dihydrochloride GSK143 dihydrochloride  Chemical Structure
  30. GC68446 NRX-103094 NRX-103094  Chemical Structure
  31. GC68445 SCD1 inhibitor-3 SCD1 inhibitor-3  Chemical Structure
  32. GC68444 SBI-993 SBI-993  Chemical Structure
  33. GC68443 T3Inh-1 T3Inh-1  Chemical Structure
  34. GC68442 L-Glutamine-15N-1 L-Glutamine-15N-1  Chemical Structure
  35. GC68441 SRI-37330 hydrochloride SRI-37330 hydrochloride  Chemical Structure
  36. GC68440 EGFR-IN-69 EGFR-IN-69  Chemical Structure
  37. GC68439 GNE-064 GNE-064  Chemical Structure
  38. GC68438 AMPA receptor modulator-3 AMPA receptor modulator-3  Chemical Structure
  39. GC68437 Vimentin-IN-1 Vimentin-IN-1  Chemical Structure
  40. GC68436 L82-G17 L82-G17  Chemical Structure
  41. GC68435 Clazosentan Clazosentan  Chemical Structure
  42. GC68433 OTS447 OTS447  Chemical Structure
  43. GC68432 DB-3-291 DB-3-291  Chemical Structure
  44. GC68431 NJH-2-030 NJH-2-030  Chemical Structure
  45. GC68430 Selatinib Selatinib  Chemical Structure
  46. GC68429 GNE-490 GNE-490  Chemical Structure
  47. GC68428 Rimantadine-d4 hydrochloride Rimantadine-d4 hydrochloride  Chemical Structure
  48. GC68427 GSK1521498 free base GSK1521498 free base  Chemical Structure
  49. GC68426 17a-Hydroxypregnenolone-d3 17a-Hydroxypregnenolone-d3  Chemical Structure
  50. GC68425 Ranolazine-d3 Ranolazine-d3  Chemical Structure
  51. GC68424 Fingolimod-d4 hydrochloride Fingolimod-d4 hydrochloride  Chemical Structure
  52. GC68423 Indomethacin-d4 Methyl Ester Indomethacin-d4 Methyl Ester  Chemical Structure
  53. GC68422 Choline-d4 chloride Choline-d4 chloride  Chemical Structure
  54. GC68421 L-Aspartic acid-13C4,15N L-Aspartic acid-13C4,15N  Chemical Structure
  55. GC68420 Propionylpromazine-d6 hydrochloride Propionylpromazine-d6 hydrochloride  Chemical Structure
  56. GC68419 Prasugrel-d3 Prasugrel-d3  Chemical Structure
  57. GC68418 Clenbuterol-d9 Clenbuterol-d9  Chemical Structure
  58. GC68417 Homovanillic acid-d5 Homovanillic acid-d5  Chemical Structure
  59. GC68416 RAD51-IN-3 RAD51-IN-3  Chemical Structure
  60. GC68415 Glycolic acid-d2 Glycolic acid-d2  Chemical Structure
  61. GC68414 (Rac)-Atropine-d3 (Rac)-Atropine-d3  Chemical Structure
  62. GC68413 CYH33 CYH33  Chemical Structure
  63. GC68412 NAMPT inhibitor-linker 1 NAMPT inhibitor-linker 1  Chemical Structure
  64. GC68411 RORγt Inverse agonist 10 RORγt Inverse agonist 10  Chemical Structure
  65. GC68410 (S)-Mirtazapine-d3 (S)-Mirtazapine-d3  Chemical Structure
  66. GC68409 Cetirizine D8 Cetirizine D8  Chemical Structure
  67. GC68408 (R)-Praziquantel-d11 (R)-Praziquantel-d11  Chemical Structure
  68. GC68407 Phenylethanolamine A-d3 Phenylethanolamine A-d3  Chemical Structure
  69. GC68405 Lys-CoA TFA Lys-CoA TFA  Chemical Structure
  70. GC68404 Human PD-L1 inhibitor IV Human PD-L1 inhibitor IV  Chemical Structure
  71. GC68403 Dusquetide Dusquetide  Chemical Structure
  72. GC68402 Danofloxacin-d3 Danofloxacin-d3  Chemical Structure
  73. GC68401 Lehmannine Lehmannine  Chemical Structure
  74. GC68399 Isolindleyin Isolindleyin  Chemical Structure
  75. GC68397 Galicaftor Galicaftor  Chemical Structure
  76. GC68396 Vepafestinib Vepafestinib  Chemical Structure
  77. GC68395 L-Isoleucine-d10 L-Isoleucine-d10  Chemical Structure
  78. GC68390 α5β1 integrin agonist-1 α5β1 integrin agonist-1  Chemical Structure
  79. GC68389 SJ995973 SJ995973  Chemical Structure
  80. GC68388 XIAP degrader-1 XIAP degrader-1  Chemical Structure
  81. GC68387 FGN849 FGN849  Chemical Structure
  82. GC68386 CD73-IN-5 CD73-IN-5  Chemical Structure
  83. GC68385 TNF-α-IN-6 TNF-α-IN-6  Chemical Structure
  84. GC68384 DL-Mevalonolactone-d7 DL-Mevalonolactone-d7  Chemical Structure
  85. GC68383 (R)-Preclamol (R)-Preclamol  Chemical Structure
  86. GC68382 L-Cysteine-1-13C L-Cysteine-1-13C  Chemical Structure
  87. GC68381 L-Glutamine-1-13C L-Glutamine-1-13C  Chemical Structure
  88. GC68380 Sarcosine-15N Sarcosine-15N  Chemical Structure
  89. GC68379 L-Arginine-13C6,15N4 hydrochloride L-Arginine-13C6,15N4 hydrochloride  Chemical Structure
  90. GC68378 GDC-4379 GDC-4379  Chemical Structure
  91. GC68377 OAB-14 OAB-14  Chemical Structure
  92. GC68376 PROTAC AR-V7 degrader-1 PROTAC AR-V7 degrader-1  Chemical Structure
  93. GC68375 Cholic acid-13C Cholic acid-13C  Chemical Structure
  94. GC68374 5a-Pregnane-3,20-dione-d6 5a-Pregnane-3,20-dione-d6  Chemical Structure
  95. GC68373 BLK-IN-2 BLK-IN-2  Chemical Structure
  96. GC68371 Mutant p53 modulator-1 Mutant p53 modulator-1  Chemical Structure
  97. GC68370 Amatuximab Amatuximab  Chemical Structure
  98. GC68369 Belantamab Belantamab  Chemical Structure
  99. GC68368 Magrolimab Magrolimab  Chemical Structure
  100. GC68367 Ieramilimab Ieramilimab  Chemical Structure
  101. GC68366 Thiocolchicine-d3 Thiocolchicine-d3  Chemical Structure

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