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(40698)
- GC81867Ac-ETDK(myr)-AMC acetatePurity: >98.00%
Ac-ETDK(myr)-AMC acetate is a DLAT-derived ε-N-myristoyllysine peptide substrate for fatty-acid deacylase HDAC11, used in fluorescence-based HDAC11 activity assays.
- GC81868Acetyl-pepstatin ammoniumPurity: >98.00%
Acetyl-pepstatin ammonium is an aspartic protease ( PRs ) inhibitor that targets HIV-1 protease and XMRV protease with K i values of 13 nM and 712 nM, respectively.
- GC81869APP669-711 acetatePurity: >98.00%
APP669-711 acetate is an N-terminally extended amyloid β peptide ( Aβ (-3)-40) that forms amyloid fibrils and co-deposits with Aβ in brain plaques, and also serves as a plasma biomarker for assessing brain Aβ load.
- GC81870Bethanidine hydriodideCAS: 2863-34-5Purity: >98.00%
Bethanidine hydriodide is an orally active antihypertensive agent and adrenergic neuron blocker.
- GC81871CAP 6 m7G(LNA)(5')ppp(5')(2'OMeA)pG trisodium solution (100 mM ± 3 mM)Purity: >98.00%
CAP 6 m7G(LNA)(5')ppp(5')(2'OMeA)pG trisodium solution (100 mM ± 3 mM) is a monomeric raw material that can be used for nucleic acid synthesis.
- GC81873Ciprofloxacin hydrochlorideCAS: 86483-48-9Purity: >98.00%
Ciprofloxacin hydrochloride (Bay-09867 hydrochloride) is an orally active, blood-brain barrier permeable fluoroquinolone antibacterial agent.
- GC81875Histone H3 (1-25), amide acetatePurity: >98.00%
Histone H3 (1-25), amide acetate is a synthetic N-terminal tail peptide derived from histone H3, which can be used to identify substrates of histone methyltransferases (HMTs).
- GC81876Imlunestrant-d₄Purity: >98.00%
Imlunestrant -d 4 (LY-3484356-d 4 ) is the deuterated-labeled Imlunestrant.
- GC81880OSU-2S TFAPurity: >98.00%
OSU-2S TFA is a non-immunosuppressive derivative of Fingolimod hydrochloride (FTY720).
- GC81882PROTAC CARM1 degrader-1 TFAPurity: >98.00%
PROTAC CARM1 degrader-1 TFA is a highly selective CARM1 PROTAC degrader, with a DC 50 of 8.1 nM in MCF‑7 cells.
- GC81883(R)-AR/BRD4 RIPTAC-1CAS: 3083307-47-2Purity: >98.00%
(R)-AR/BRD4 RIPTAC-1 is the R-enantiomer of AR/BRD4 RIPTAC-1.
- GC81884(R)-Vanzacaftor-d₄Purity: >98.00%
(R)-Vanzacaftor -d 4 ((R)-VX-121-d 4 ) is the deuterated-labeled (R)-Vanzacaftor.
- GC81886(S)-PhenylpiracetamCAS: 949925-08-0Purity: >98.00%
(S)-Phenylpiracetam ((S)-Carphedon; (S)-Fonturacetam; (S)-MRZ 9547) is an orally active and selective dopamine transporter inhibitor, with K i = 56 μM.
- GC81890Temozolomide-¹⁵NPurity: >98.00%
Temozolomide - 15 N (NSC 362856- 15 N) is the 15 N-labeled Temozolomide.
- GC81891Tri-GalNAc-NH2CAS: 1646198-77-7Purity: >98.00%
Tri-GalNAc-NH2 is a synthetic tri-N-acetylgalactosamine ligand that targets the asialoglycoprotein receptor (ASGPR).
- GC81892Vevorisertib tetrahydrochloridePurity: >98.00%
Vevorisertib tetrahydrochloride (ARQ 751 tetrahydrochloride) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation.
- GC81893Rfamide TFAPurity: >99.50%
Rfamide TFA (Arginylphenylalaninamide TFA) is a neuropeptide that has contraction-inducing activity in gastropod muscles.
- GC81894Adamantan-2-amineCAS: 13074-39-0Purity: >98.00%
Adamantan-2-amine (2-Aminoadamantane) serves as the hydrophobic tag structural unit of Tubulin degrader 2 and is used for the synthesis of anticancer drugs that target tubulin via a dual mechanism.
- GC81895RB 101 hydrochloridePurity: >98.00%
RB 101 hydrochloride is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor.
- GC81897HaloAUTAC tt15CAS: 2241668-45-9Purity: >96.00%
HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC), that targets the Halo Tag carrying proteins, and degrades via the autophagy mechanism.
- GC81900CP61 acetatePurity: >98.50%
CP61 acetate is a CtBP1 and CtBP2 inhibitor that binds to dimeric CtBP1 and allosterically inhibits NADH binding, disrupting the NADH -dependent dimerization of CtBP1 and CtBP2, inducing aberrant mitosis and micronucleus formation, thereby inhibiting cell proliferation and colony formation.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81867 | Ac-ETDK(myr)-AMC acetate | - | >98.00% | |
Ac-ETDK(myr)-AMC acetate is a DLAT-derived ε-N-myristoyllysine peptide substrate for fatty-acid deacylase HDAC11, used in fluorescence-based HDAC11 activity assays. | ||||
| GC81868 | Acetyl-pepstatin ammonium | - | >98.00% | |
Acetyl-pepstatin ammonium is an aspartic protease ( PRs ) inhibitor that targets HIV-1 protease and XMRV protease with K i values of 13 nM and 712 nM, respectively. | ||||
| GC81869 | APP669-711 acetate | - | >98.00% | |
APP669-711 acetate is an N-terminally extended amyloid β peptide ( Aβ (-3)-40) that forms amyloid fibrils and co-deposits with Aβ in brain plaques, and also serves as a plasma biomarker for assessing brain Aβ load. | ||||
| GC81870 | Bethanidine hydriodide | 2863-34-5 | >98.00% | |
Bethanidine hydriodide is an orally active antihypertensive agent and adrenergic neuron blocker. | ||||
| GC81871 | CAP 6 m7G(LNA)(5')ppp(5')(2'OMeA)pG trisodium solution (100 mM ± 3 mM) | - | >98.00% | |
CAP 6 m7G(LNA)(5')ppp(5')(2'OMeA)pG trisodium solution (100 mM ± 3 mM) is a monomeric raw material that can be used for nucleic acid synthesis. | ||||
| GC81872 | CPTH2-d₄ | - | >98.00% | |
CPTH2 -d 4 is the deuterated-labeled CPTH2. | ||||
| GC81873 | Ciprofloxacin hydrochloride | 86483-48-9 | >98.00% | |
Ciprofloxacin hydrochloride (Bay-09867 hydrochloride) is an orally active, blood-brain barrier permeable fluoroquinolone antibacterial agent. | ||||
| GC81875 | Histone H3 (1-25), amide acetate | - | >98.00% | |
Histone H3 (1-25), amide acetate is a synthetic N-terminal tail peptide derived from histone H3, which can be used to identify substrates of histone methyltransferases (HMTs). | ||||
| GC81876 | Imlunestrant-d₄ | - | >98.00% | |
Imlunestrant -d 4 (LY-3484356-d 4 ) is the deuterated-labeled Imlunestrant. | ||||
| GC81879 | NCP26 TFA | - | >99.50% | |
NCP26 TFA is an ATP-competitive ProRS inhibitor (with a K D of 271 nM in the absence of proline, and a K D of 0.35 nM in the presence of 100 μM proline). | ||||
| GC81880 | OSU-2S TFA | - | >98.00% | |
OSU-2S TFA is a non-immunosuppressive derivative of Fingolimod hydrochloride (FTY720). | ||||
| GC81882 | PROTAC CARM1 degrader-1 TFA | - | >98.00% | |
PROTAC CARM1 degrader-1 TFA is a highly selective CARM1 PROTAC degrader, with a DC 50 of 8.1 nM in MCF‑7 cells. | ||||
| GC81883 | (R)-AR/BRD4 RIPTAC-1 | 3083307-47-2 | >98.00% | |
(R)-AR/BRD4 RIPTAC-1 is the R-enantiomer of AR/BRD4 RIPTAC-1. | ||||
| GC81884 | (R)-Vanzacaftor-d₄ | - | >98.00% | |
(R)-Vanzacaftor -d 4 ((R)-VX-121-d 4 ) is the deuterated-labeled (R)-Vanzacaftor. | ||||
| GC81886 | (S)-Phenylpiracetam | 949925-08-0 | >98.00% | |
(S)-Phenylpiracetam ((S)-Carphedon; (S)-Fonturacetam; (S)-MRZ 9547) is an orally active and selective dopamine transporter inhibitor, with K i = 56 μM. | ||||
| GC81890 | Temozolomide-¹⁵N | - | >98.00% | |
Temozolomide - 15 N (NSC 362856- 15 N) is the 15 N-labeled Temozolomide. | ||||
| GC81891 | Tri-GalNAc-NH2 | 1646198-77-7 | >98.00% | |
Tri-GalNAc-NH2 is a synthetic tri-N-acetylgalactosamine ligand that targets the asialoglycoprotein receptor (ASGPR). | ||||
| GC81892 | Vevorisertib tetrahydrochloride | - | >98.00% | |
Vevorisertib tetrahydrochloride (ARQ 751 tetrahydrochloride) is an orally active allosteric AKT inhibitor that blocks AKT phosphorylation. | ||||
| GC81893 | Rfamide TFA | - | >99.50% | |
Rfamide TFA (Arginylphenylalaninamide TFA) is a neuropeptide that has contraction-inducing activity in gastropod muscles. | ||||
| GC81894 | Adamantan-2-amine | 13074-39-0 | >98.00% | |
Adamantan-2-amine (2-Aminoadamantane) serves as the hydrophobic tag structural unit of Tubulin degrader 2 and is used for the synthesis of anticancer drugs that target tubulin via a dual mechanism. | ||||
| GC81895 | RB 101 hydrochloride | - | >98.00% | |
RB 101 hydrochloride is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. | ||||
| GC81897 | HaloAUTAC tt15 | 2241668-45-9 | >96.00% | |
HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC), that targets the Halo Tag carrying proteins, and degrades via the autophagy mechanism. | ||||
| GC81898 | LLC355 | - | >99.50% | |
LLC355 is a discoidin domain receptor 1 ( DDR1 ) ATTEC degrader with a DC 50 of 150.8 nM. | ||||
| GC81900 | CP61 acetate | - | >98.50% | |
CP61 acetate is a CtBP1 and CtBP2 inhibitor that binds to dimeric CtBP1 and allosterically inhibits NADH binding, disrupting the NADH -dependent dimerization of CtBP1 and CtBP2, inducing aberrant mitosis and micronucleus formation, thereby inhibiting cell proliferation and colony formation. | ||||
