A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Ki values of 4 and 264 nM, respectively[1].
A2A receptor antagonist 1 (CPI-444 analog) is a potent adenosine A2A receptor antagonist, selective over the A1 receptor and demonstrates its binding activity with Ki values of 4 and 264 nM, respectively[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
309.30
Formula
C16H12FN5O
CAS 号
443103-97-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Gillespie RJ, et al. Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines. Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9.
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors[1][2].
体外研究 (In Vitro)
Estrogen receptor modulator 1 (compound 18) (100 nM; 10 days) inhibits T47D:A18/PKCα and T47D:A18-TAM1 colony formation[2]. Estrogen receptor modulator 1 (100 nM; 9 days) significantly inhibits the growth of MCF-7:5C cell, and induces apoptosis in these cells 6 days[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[2]
Cell Line:
T47D:A18/PKCα and T47D:A18-TAM1 cells
Concentration:
100 nM
Incubation Time:
10 days
Result:
Inhibit T47D:A18/PKCα and T47D:A18-TAM1 colony formation.
Cell Viability Assay[2]
Cell Line:
MCF-7:5C cells
Concentration:
100 nM
Incubation Time:
9 days
Result:
Significantly inhibited the growth of MCF-7:5C cells.
体内研究 (In Vivo)
Estrogen receptor modulator 1 (1.5 mg/animal; p.o. ; daily for 2 weeks) results in regression of T47D:A18/PKCα tumors[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
4-6 week old athymic mice (Harlan-Sprague-Dawley)[2]
Dosage:
1.5 mg/animal
Administration:
p.o. ; daily for 2 weeks
Result:
Significantly reduced tumor volume.
分子量
242.29
Formula
C14H10O2S
CAS 号
63676-22-2
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]. Brogi S, et al. 3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors. Eur J Med Chem. 2013 Sep;67:344-51.
[2]. Molloy ME, et al. Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer. Mol Cancer Ther. 2014 Nov;13(11):2515-26.
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].
IC50 & Target
IC50: 59 nM (androgen receptor)[1]
体外研究 (In Vitro)
Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 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.
Cell Proliferation Assay[1]
Cell Line:
Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145)
Concentration:
1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM
Incubation Time:
7 days
Result:
Antiproliferative effects of in LNCAP and LNAR cells.
体内研究 (In Vivo)
Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model[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.
Animal Model:
Male athymic nude mice with LNCaP xenograft model of CRPC[1]
Dosage:
100 mg/kg
Administration:
Orally once a day for 5 weeks
Result:
Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.
分子量
416.90
Formula
C21H25ClN4O3
CAS 号
1338812-36-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704.
[2]. Han X, et al. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 24;62(2):941-964.
This peptide derived from the ligand binding site of the human gamma-interferon (IFN-gamma) receptor is an antagonist of human IFN-gamma. It inhibited human IFN-gamma-induced expression of HLR/DR antigen on Colo 205 cells with an approximate IC50 of 35 碌M. Immobilized peptide specifically bound recombinant human IFN-gamma. Tyrosine substitution at residue 121 allowed facile quantification and conjugation of the peptide.
溶解度
分子量
886
化学式
C35H59N13O12S1
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
An LRF-amide motif containing fragment of malignant melanoma metastasis suppressor KiSs-1. It bound with low nanomolar affinity to the rat and human G protein-coupled receptor GPR54 expressed in Chinese hamster ovary K1 cells and stimulated PIP2 hydrolysis, Ca2+ mobilization, arachidonic acid release, ERK1/2 and p38 MAP kinase phosphorylation, and stress fiber formation but inhibited cell proliferation.
溶解度
分子量
2668.88
化学式
C114H174N30O42S1
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
D.P.Bottaro et al., J. Biol. Chem., 268, 9180 (1993)
EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer[1].
IC50 & Target[1]
EP4
分子量
498.52
Formula
C26H21F3N2O3S
CAS 号
1207954-34-4
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]. Wei W. Yuan, et al. Heterocyclic amide derivatives as ep4 receptor antagonists. Patent WO2010019796A1.
EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer[1].
IC50 & Target[1]
EP4
分子量
498.52
Formula
C26H21F3N2O3S
CAS 号
1207954-34-4
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]. Wei W. Yuan, et al. Heterocyclic amide derivatives as ep4 receptor antagonists. Patent WO2010019796A1.
EP4 receptor antagonist 3 is a potent EP4 receptor antagonist, example 3,extracted from patent WO2010019796 A1. EP4 receptor antagonist 3 can be used for the reseacrh of EP4 receptor-mediated diseases, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer[1].
IC50 & Target[1]
EP4
分子量
498.52
Formula
C26H21F3N2O3S
CAS 号
1207954-34-4
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]. Wei W. Yuan, et al. Heterocyclic amide derivatives as ep4 receptor antagonists. Patent WO2010019796A1.