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方案
≥98% (HPLC)
表单
powder
颜色
white to brownish
溶解性
DMSO: 2 mg/mL to clear
运输
ambient
储存温度
2-8°C
SMILES字符串
O=C(N1CCC)NC2=C(N=C(C3=CC=C(S(=O)(N4CCN(C5=CC=C(Cl)C=C5)CC4)=O)C=C3)N2)C1=O
InChI
1S/C24H25ClN6O4S/c1-2-11-31-23(32)20-22(28-24(31)33)27-21(26-20)16-3-9-19(10-4-16)36(34,35)30-14-12-29(13-15-30)18-7-5-17(25)6-8-18/h3-10H,2,11-15H2,1H3,(H,26,27)(H,28,33)
InChI key
OVHCTHHFOHMNFV-UHFFFAOYSA-N
生化/生理作用
A high-affinity, selective antagonist against A2b adenosine receptor (A2b-AR, A2bR).
PSB-603 is an adenosine receptor A2b antagonist (IC50 = 1.13 nM against 10 μM A2bR agonist NECA-induced calcium response in Jurkat T cells in the presence of 200 nM A2aR antagonist MSX-2) that targets A2bR with high affinity (KD = 0.403 nM/human, 0.457 nM/rat, 4.09 nM/mouse A2bR; Ki against 0.3 nM [3H]PSB-603 = 0.553 nM/human, 0.355 nM/rat, 0.265 nM/mouse A2bR) and selectivity, exhibiting little affinity toward A1, A2a, or A3 adenosine receptors by competition binding assay (Ki >10 μM against 0.4 nM [3H]DPCPX for human/rat A1R, 1 nM [3H]MSX-2 for human/mouse/rat A2aR, 10 nM [3H]NECA for human/mouse/rat A3R) with the exception of mouse A1R (Ki = 42.2 nM against 0.4 nM [3H]DPCPX).
PSB-603 is known to modify cellular metabolism and enhance cellular sensitivity for chemotherapy. Thus, PSB-603 is recognized to possess anticancer action, which has been studied in colorectal cancer.
警示用语：
Warning
危险声明
危险分类
Skin Irrit. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Christina Mølck et al.
Cancer letters, 383(1), 135-143 (2016-10-30)
Adenosine is a multifaceted regulator of tumor progression. It modulates immune cell activity as well as acting directly on tumor cells. The A The A PSB-603 alters cellular metabolism in colorectal cancer cells and increases their sensitivity to chemotherapy. Although
Mohamad Wessam Alnouri et al.
Purinergic signalling, 11(3), 389-407 (2015-07-02)
Adenosine receptors (ARs) have emerged as new drug targets. The majority of data on affinity/potency and selectivity of AR ligands described in the literature has been obtained for the human species. However, preclinical studies are mostly performed in mouse or
The A2b adenosine receptor antagonist PSB-603 promotes oxidative phosphorylation and ROS production in colorectal cancer cells via adenosine receptor-independent mechanism.
M?lck C, et al.
Cancer Letters, 383(1), 135-143 (2016)
Denis Chang et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(44), 27502-27508 (2020-10-23)
Cyclic dinucleotides (CDNs) are secondary messengers used by prokaryotic and eukaryotic cells. In mammalian cells, cytosolic CDNs bind STING (stimulator of IFN gene), resulting in the production of type I IFN. Extracellular CDNs can enter the cytosol through several pathways
Thomas Borrmann et al.
Journal of medicinal chemistry, 52(13), 3994-4006 (2009-07-03)
A new series of 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines was designed, synthesized, and characterized in radioligand binding and functional assays at A(2B) adenosine receptors. A(2B) antagonists with subnanomolar affinity and high selectivity were discovered. The most potent compounds were 1-ethyl-8-(4-(4-(4-trifluoromethylbenzyl)piperazine-1-sulfonyl)phenyl)xanthine (24, PSB-09120, K(i) (human
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