TLR7/8 agonist 4 hydroxy-PEG10-acid Chemical Structure
CAS No. : 2388520-17-8
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the cleavable ADC linker hydroxy-PEG10-acid (HY-133307)[1].
IC50 & Target[1]
Traditional Cytotoxic Agents
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
837.01
Formula
C41H68N6O12
CAS 号
2388520-17-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Shelley Erin ACKERMAN, et al. Immunoconjugates targeting her2. WO2020190725A1.
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function[1].
IC50 & Target
IC50: 20 nM (STING agonist-4)[1]
体外研究 (In Vitro)
STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC50 of 3.1 μM[1]. STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (Kd) of approximately 1.6 nM[1]. STING agonist-4 (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC50 of 53.9 μM[1]. STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
Human peripheral blood mononuclear cells (PBMCs)
Concentration:
0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM
Incubation Time:
2 hours
Result:
Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β.
分子量
678.74
Formula
C34H38N12O4
CAS 号
2138300-40-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 10 mg/mL (14.73 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
*STING agonist-4 is usually formulated as a suspension.
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride Chemical Structure
CAS No. : 2388520-36-1
规格
是否有货
100 mg
询价
250 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the cleavable ADC linker hydroxy-PEG10-acid (HY-133307)[1].
IC50 & Target[1]
Traditional Cytotoxic Agents
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
873.47
Formula
C41H69ClN6O12
CAS 号
2388520-36-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Shelley Erin ACKERMAN, et al. Immunoconjugates targeting her2. WO2020190725A1.
[1]. Behrendt HJ, et al. Characterization of the mouse cold-menthol receptor TRPM8 and vanilloid receptor type-1 VR1 using a fluorometric imaging plate reader (FLIPR) assay. Br J Pharmacol. 2004 Feb;141(4):737-45.
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells[1].
体外研究 (In Vitro)
CB2 receptor agonist 3 (Compound 2a) is also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
440.36
Formula
C24H23Cl2N3O
CAS 号
919077-81-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Murineddu G, et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2′,4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2006;49(25):7502-7512.
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells[1].
体外研究 (In Vitro)
CB2 receptor agonist 3 (Compound 2a) is also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
440.36
Formula
C24H23Cl2N3O
CAS 号
919077-81-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Murineddu G, et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2′,4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2006;49(25):7502-7512.
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells[1].
体外研究 (In Vitro)
CB2 receptor agonist 3 (Compound 2a) is also shown to be agonist in an in vitro model based on human promyelocytic leukemia HL-60 cells[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
440.36
Formula
C24H23Cl2N3O
CAS 号
919077-81-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Murineddu G, et al. Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2′,4′-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J Med Chem. 2006;49(25):7502-7512.
EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB[1].
体外研究 (In Vitro)
EphA2 agonist 2 (Lead compound) shows antiproliferation activity with IC50 values of 2.1 ± 1.05 μM and 5.2 ± 2.56 μM against U251 EphA2 overexpressed and U251 wild type cells, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
772.94
Formula
C40H56N10O6
CAS 号
2169273-66-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Orahoske CM, et al. Dimeric small molecule agonists of EphA2 receptor inhibit glioblastoma cell growth. Bioorg Med Chem. 2020 Sep 15;28(18):115656.
Nurr1 agonist 1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.
分子量
266.29
Formula
C16H14N2O2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zaienne D, et al. Development and Profiling of Inverse Agonist Tools for the Neuroprotective Transcription Factor Nurr1. J Med Chem. 2021 Oct 28;64(20):15126-15140.
Nurr1 agonist 1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.
分子量
266.29
Formula
C16H14N2O2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zaienne D, et al. Development and Profiling of Inverse Agonist Tools for the Neuroprotective Transcription Factor Nurr1. J Med Chem. 2021 Oct 28;64(20):15126-15140.
Nurr1 agonist 1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.
分子量
266.29
Formula
C16H14N2O2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zaienne D, et al. Development and Profiling of Inverse Agonist Tools for the Neuroprotective Transcription Factor Nurr1. J Med Chem. 2021 Oct 28;64(20):15126-15140.
EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation[1].
IC50 & Target
EphA2[1]
体外研究 (In Vitro)
EphA2 agonist 1 (Compound 7bg) inhibits cell proliferation with IC50 values of 1.90 ± 0.55 μM and 7.91 ± 2.28 μM against U251 EphA2 overexpressed and U251 wild type cells, respectively[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1019.07
Formula
C50H58N12O12
CAS 号
2611459-57-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Orahoske CM, et al. Dimeric small molecule agonists of EphA2 receptor inhibit glioblastoma cell growth. Bioorg Med Chem. 2020 Sep 15;28(18):115656.
TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders[1].
分子量
417.50
Formula
C24H27N5O2
CAS 号
2115702-83-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yang M, et al. Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs. Bioorg Med Chem Lett. 2022;59:128548.
TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders[1].
分子量
417.50
Formula
C24H27N5O2
CAS 号
2115702-83-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yang M, et al. Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs. Bioorg Med Chem Lett. 2022;59:128548.
TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders[1].
分子量
417.50
Formula
C24H27N5O2
CAS 号
2115702-83-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yang M, et al. Toll-like receptor 7 and 8 imidazoquinoline-based agonist/antagonist pairs. Bioorg Med Chem Lett. 2022;59:128548.
GLP-1R agonist 4 is a potent agonist of GLP-1R. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 4 has the potential for the research of diabetes (extracted from patent WO2019239319A1, compound 96)[1].
分子量
610.05
Formula
C32H30ClF2N3O5
CAS 号
2401894-26-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Gary Erik Aspnes, et al. Glp-1 receptor agonists and uses thereof. Patent WO2019239319A1.