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(40823)
- GC814672,6-Dibromo-4-(hydroxymethyl)phenolCAS: 2316-62-3Purity: >98.00%
2,6-Dibromo-4-(hydroxymethyl) phenol (Compound 5) acts as a selective inhibitor of Saccharomyces cerevisiae glucose-6-phosphate dehydrogenase, with an IC 50 value of 50.2 μM, and shows no activity against Leuconostoc mesenteroides glucose-6-phosphate dehydrogenase [1] .
- GC81469Morpholino-G(N-iBu) PhosphoramiditeCAS: 956139-25-6Purity: >98.00%
Morpholino-G(N-iBu) Phosphoramidite is a guanine-containing morpholino phosphoramidite building block with an isobutyryl (iBu)-protected guanine amino group.
- GC81470DMT-NH-PEG4-phosphoramiditeCAS: 3099406-90-0Purity: >98.00%
1,1-Bis(4-methoxyphenyl)-1-phenyl-3,6,9,12-tetraoxa-2-azatetradecan-14-yl (2-cyanoethyl) diisopropylphosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
- GC81471β-L-dT-CE phosphoramiditeCAS: 141846-55-1Purity: >98.00%
β-L-dT-CE phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
- GC81472pdU-CE PhosphoramiditeCAS: 198080-43-2Purity: >98.00%
pdU-CE Phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
- GC81473Amino-modifier-C6-dC CEPCAS: 853955-92-7Purity: >98.00%
(2R,3S,5R)-2-((Bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-5-(4-(((dimethylamino)methylene)amino)-2-oxo-5-(3-oxo-3-((6-(2,2,2-trifluoroacetamido)hexyl)amino)prop-1-en-1-yl)pyrimidin-1(2H)-yl)tetrahydrofuran-3-yl (2-cyanoethyl) diisopropylphosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
- GC814744'-O-CH2-phosphate methyl ester-2'-O-Me-rU-3'-CE-phosphoramiditeCAS: 2197181-94-3Purity: >98.00%
4'-O-CH2-phosphate methyl ester-2'-O-Me-rU-3'-CE-phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis.
- GC81475Thiol-modifier C6 S-S CE phosphoramiditeCAS: 148254-21-1Purity: >98.00%
Thiol-modifier C6 S-S CE phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis.
- GC81476DMTr-2'-O-Propargyl-rU-3'-CE-phosphoramiditeCAS: 171486-62-7Purity: >98.00%
DMTr-2'-O-propargyl-rU-3'-CE -Phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis.
- GC81477DMTr-2'-O-C16-rU-3'-CE-phosphoramiditeCAS: 2382942-83-6Purity: >98.00%
DMTr-2'-O-C16-rU-3'-CE-Phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis.
- GC81478DMTr-2'-O-Me-rA(Bz)-3'-(D)-PSM-phosphoramiditeCAS: 2379296-27-0Purity: >98.00%
DMTr-2'-O-Me-rA(Bz)-3'-(D)-PSM-phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis.
- GC81479SMARCA2-IN-10CAS: 82131-85-9Purity: >96.00%
SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor ( IC 50 =17.676 μM).
- GC81482PF-07976016CAS: 3059496-70-4Purity: >98.00%
PF-07976016 (GIPR antagonist 4) is an orally active GIPR antagonist with an IC 50 of 4.1 nM.
- GC81486Anti-Mouse CD370 Antibody (1F6)Purity: >97.50%
Anti-Mouse CD370 Antibody (1F6) reacts with the mouse CD370 (also known as CLEC9A or DNGR1).
- GC81487Phlorofucofuroeckol ACAS: 128129-56-6Purity: >98.00%
Phlorofucofuroeckol A is a FcεRI inhibitor with low cytotoxicity toward basophilic leukemia cells.
- GC81490SYN1327 acetatePurity: >98.00%
SYN1327 acetate is a potent monomeric cyclic competitive antagonistic peptide targeting the neonatal Fc receptor ( FcRn ), with a K d of 31 nM for human FcRn at pH 6 and a K d of 170 nM at pH 7.4.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81467 | 2,6-Dibromo-4-(hydroxymethyl)phenol | 2316-62-3 | >98.00% | |
2,6-Dibromo-4-(hydroxymethyl) phenol (Compound 5) acts as a selective inhibitor of Saccharomyces cerevisiae glucose-6-phosphate dehydrogenase, with an IC 50 value of 50.2 μM, and shows no activity against Leuconostoc mesenteroides glucose-6-phosphate dehydrogenase [1] . | ||||
| GC81468 | MS102 | 3058587-77-9 | >98.00% | |
MS102 is an orally active ubiquitin specific peptidase 2 ( USP2 ) inhibitor with an IC 50 of 5.46 μM. | ||||
| GC81469 | Morpholino-G(N-iBu) Phosphoramidite | 956139-25-6 | >98.00% | |
Morpholino-G(N-iBu) Phosphoramidite is a guanine-containing morpholino phosphoramidite building block with an isobutyryl (iBu)-protected guanine amino group. | ||||
| GC81470 | DMT-NH-PEG4-phosphoramidite | 3099406-90-0 | >98.00% | |
1,1-Bis(4-methoxyphenyl)-1-phenyl-3,6,9,12-tetraoxa-2-azatetradecan-14-yl (2-cyanoethyl) diisopropylphosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides. | ||||
| GC81471 | β-L-dT-CE phosphoramidite | 141846-55-1 | >98.00% | |
β-L-dT-CE phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides. | ||||
| GC81472 | pdU-CE Phosphoramidite | 198080-43-2 | >98.00% | |
pdU-CE Phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides. | ||||
| GC81473 | Amino-modifier-C6-dC CEP | 853955-92-7 | >98.00% | |
(2R,3S,5R)-2-((Bis(4-methoxyphenyl)(phenyl)methoxy)methyl)-5-(4-(((dimethylamino)methylene)amino)-2-oxo-5-(3-oxo-3-((6-(2,2,2-trifluoroacetamido)hexyl)amino)prop-1-en-1-yl)pyrimidin-1(2H)-yl)tetrahydrofuran-3-yl (2-cyanoethyl) diisopropylphosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides. | ||||
| GC81474 | 4'-O-CH2-phosphate methyl ester-2'-O-Me-rU-3'-CE-phosphoramidite | 2197181-94-3 | >98.00% | |
4'-O-CH2-phosphate methyl ester-2'-O-Me-rU-3'-CE-phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis. | ||||
| GC81475 | Thiol-modifier C6 S-S CE phosphoramidite | 148254-21-1 | >98.00% | |
Thiol-modifier C6 S-S CE phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis. | ||||
| GC81476 | DMTr-2'-O-Propargyl-rU-3'-CE-phosphoramidite | 171486-62-7 | >98.00% | |
DMTr-2'-O-propargyl-rU-3'-CE -Phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis. | ||||
| GC81477 | DMTr-2'-O-C16-rU-3'-CE-phosphoramidite | 2382942-83-6 | >98.00% | |
DMTr-2'-O-C16-rU-3'-CE-Phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis. | ||||
| GC81478 | DMTr-2'-O-Me-rA(Bz)-3'-(D)-PSM-phosphoramidite | 2379296-27-0 | >98.00% | |
DMTr-2'-O-Me-rA(Bz)-3'-(D)-PSM-phosphoramidite is a monomeric raw material that can be used for nucleic acid synthesis. | ||||
| GC81479 | SMARCA2-IN-10 | 82131-85-9 | >96.00% | |
SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor ( IC 50 =17.676 μM). | ||||
| GC81480 | FHD-909 | 3008577-34-9 | >98.00% | |
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. | ||||
| GC81481 | SKLB06489 | - | >98.00% | |
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC 50 values of 64.55 nM ( PRMT1 ), 4.21 nM ( PRMT6 ), and 51.27 nM ( PRMT8 ). | ||||
| GC81482 | PF-07976016 | 3059496-70-4 | >98.00% | |
PF-07976016 (GIPR antagonist 4) is an orally active GIPR antagonist with an IC 50 of 4.1 nM. | ||||
| GC81483 | AKIR001 | - | >99.00% | |
AKIR001 is a high-affinity human IgG1 antibody targeting CD44v6. | ||||
| GC81484 | (R)-MMG-1 | 2064030-22-2 | >98.00% | |
(R)-MMG-1 is the R-enantiomer of MMG-1. | ||||
| GC81485 | C201-0243 | 931360-60-0 | >99.50% | |
C201-0243 is a FcRn antagonist. | ||||
| GC81486 | Anti-Mouse CD370 Antibody (1F6) | - | >97.50% | |
Anti-Mouse CD370 Antibody (1F6) reacts with the mouse CD370 (also known as CLEC9A or DNGR1). | ||||
| GC81487 | Phlorofucofuroeckol A | 128129-56-6 | >98.00% | |
Phlorofucofuroeckol A is a FcεRI inhibitor with low cytotoxicity toward basophilic leukemia cells. | ||||
| GC81488 | Z223-2027 | 1359344-58-3 | >98.00% | |
Z223-2027 is a FcRn inhibitor. | ||||
| GC81489 | SYN1327 | 1020264-43-0 | >99.50% | |
SYN1327 is a potent monomeric cyclic competitive antagonistic peptide targeting the neonatal Fc receptor ( FcRn ), with a K d of 31 nM for human FcRn at pH 6 and a K d of 170 nM at pH 7.4. | ||||
| GC81490 | SYN1327 acetate | - | >98.00% | |
SYN1327 acetate is a potent monomeric cyclic competitive antagonistic peptide targeting the neonatal Fc receptor ( FcRn ), with a K d of 31 nM for human FcRn at pH 6 and a K d of 170 nM at pH 7.4. | ||||