Signaling Pathways
Research Area, Signaling Pathways | GlpBio Life Science Products Suppliers
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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)
- GC81019BTR2000 TFAPurity: >98.50%
BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity.
- GC81020JNK1 ligand-1-NH-Ph-COOHCAS: 3047792-63-9Purity: >98.00%
JNK1 ligand-1 (Compound P1) is a selective JNK1 inhibitor.
- GC81021p38α ligand-1CAS: 586379-64-8Purity: >98.50%
P38α ligand-1 is a p38α ligand that can be used for the synthesis of PROTACs, such as NR-7h [1] .
- GC81024PROTAC RNF4 degrader-1Purity: >98.00%
PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader ( K d = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system.
- GC81026PROTAC SKP2 Degrader-1CAS: 3120650-15-6Purity: >99.50%
PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K d value of 6.28 μM.
- GC81027PROTAC HIF-1α degrader-2CAS: 3095636-64-6Purity: >98.00%
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex.
- GC81029MRT-31619 formatePurity: >99.00%
MRT-31619 formate is a molecular gel degrader (MGD) targeting CRBN.
- GC81032Z6466608628 hydrochloridePurity: >99.00%
Z6466608628 hydrochloride is a selective PPIL4 molecular glue degrader with human PPIL4 EC 50 values of 0.34 µM.
- GC81033CoREST/LSD1 degrader-1Purity: >99.00%
CoREST/LSD1 degrader-1 (Compound 4) is a molecular glue degrader targeting the KBTBD4 E3 ubiquitin ligase.
- GC81036PROTAC AAK1 degrader-1CAS: 3113123-63-7Purity: >98.00%
PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC 50 of <10 nM.
- GC81038PROTAC mHTT Degrader-1CAS: 2919475-43-5Purity: >98.00%
PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin ( mHTT ) PROTAC degrader.
- GC81039PROTAC MALT1 Degrader-1CAS: 2975664-37-8Purity: >98.00%
PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader.
- GC81042PI3K/mTOR ligand-1CAS: 1197160-66-9Purity: >97.00%
PI3K/mTOR ligand-1 is a ligand for the target protein of PROTAC ( PI3K / mTOR ).
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81019 | BTR2000 TFA | - | >98.50% | |
BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. | ||||
| GC81020 | JNK1 ligand-1-NH-Ph-COOH | 3047792-63-9 | >98.00% | |
JNK1 ligand-1 (Compound P1) is a selective JNK1 inhibitor. | ||||
| GC81021 | p38α ligand-1 | 586379-64-8 | >98.50% | |
P38α ligand-1 is a p38α ligand that can be used for the synthesis of PROTACs, such as NR-7h [1] . | ||||
| GC81022 | JWZ-8-103 | 3110272-60-8 | >98.00% | |
JWZ-8-103 is an orally active analog of PRLX-93936 and a molecular glue targeting TRIM21. | ||||
| GC81023 | 5-Iodo-BIIB021 | 911397-54-1 | >98.00% | |
5-Iodo-BIIB021 is a HSP90 ligand. | ||||
| GC81024 | PROTAC RNF4 degrader-1 | - | >98.00% | |
PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader ( K d = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. | ||||
| GC81025 | PSP-0119 | 3104855-98-0 | >98.50% | |
PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 ( IC 50 = 2.83 nM). | ||||
| GC81026 | PROTAC SKP2 Degrader-1 | 3120650-15-6 | >99.50% | |
PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K d value of 6.28 μM. | ||||
| GC81027 | PROTAC HIF-1α degrader-2 | 3095636-64-6 | >98.00% | |
PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. | ||||
| GC81028 | MRT-31619 | - | >98.00% | |
MRT-31619 is a selective CRBN Molecular glue degrader, with an IC 50 of 14 nM and an EC 50 of 72 nM. | ||||
| GC81029 | MRT-31619 formate | - | >99.00% | |
MRT-31619 formate is a molecular gel degrader (MGD) targeting CRBN. | ||||
| GC81030 | XMU-MP-8 | 2271314-01-1 | >99.00% | |
XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. | ||||
| GC81031 | NEO-811 | 3084635-77-5 | >98.00% | |
NEO-811 is a selective and orally active ARNT (HIF-1β) molecular glue degrader. | ||||
| GC81032 | Z6466608628 hydrochloride | - | >99.00% | |
Z6466608628 hydrochloride is a selective PPIL4 molecular glue degrader with human PPIL4 EC 50 values of 0.34 µM. | ||||
| GC81033 | CoREST/LSD1 degrader-1 | - | >99.00% | |
CoREST/LSD1 degrader-1 (Compound 4) is a molecular glue degrader targeting the KBTBD4 E3 ubiquitin ligase. | ||||
| GC81034 | YSA64 | - | >98.00% | |
YSA64 is an orally active RBM39 -targeting molecular glue. | ||||
| GC81035 | TNG961 | 3127009-52-0 | >98.50% | |
TNG961 is a selective and orally active CRBN-mediated HBS1L molecular glue degrader. | ||||
| GC81036 | PROTAC AAK1 degrader-1 | 3113123-63-7 | >98.00% | |
PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC 50 of <10 nM. | ||||
| GC81037 | AP-7-168 | 2816062-15-2 | >99.50% | |
AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor ( β2AR ). | ||||
| GC81038 | PROTAC mHTT Degrader-1 | 2919475-43-5 | >98.00% | |
PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin ( mHTT ) PROTAC degrader. | ||||
| GC81039 | PROTAC MALT1 Degrader-1 | 2975664-37-8 | >98.00% | |
PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader. | ||||
| GC81040 | VVD 065 | 3034876-85-9 | >99.50% | |
VVD 065 is an orally active KEAP1 -dependent NRF2 molecular glue degrader with a KEAP1 K D of 65 nM. | ||||
| GC81041 | GP262 | 3107761-81-6 | >98.50% | |
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC 50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. | ||||
| GC81042 | PI3K/mTOR ligand-1 | 1197160-66-9 | >97.00% | |
PI3K/mTOR ligand-1 is a ligand for the target protein of PROTAC ( PI3K / mTOR ). | ||||