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PD 168368
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD 168368图片
CAS NO:204066-82-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PD 168368 是一种有效的、竞争性的选择性神经调节蛋白 B 受体 (NMB-R) 拮抗剂,Ki为 15-45 nM。 PD 168368 是神经调节素 B 受体(NMBR; IC50=96 nM)和胃泌素释放肽受体 (GRPR; IC50=3500 nM))的双重拮抗剂。PD 168368 还是一种FPR1/FPR2/FPR3的混合激动剂,EC50分别为 0.57、0.24 和 2.7 nM。
生物活性

PD 168368 is a potent, competitive, and selectiveneuromedin B receptor(NMB-R) antagonist with theKiof 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR;IC50=96 nM) / gastrin-releasing peptide receptor (GRPRIC50=3500 nM) antagonist[2]. PD 168368 also is a mixedFPR1/FPR2/FPR3agonist withEC50s of 0.57, 0.24, and 2.7 nM, respectively[3].

体外研究
(In Vitro)

PD 168368 (PD168368) is highly active and stimulated [Ca2+]Irelease in human neutrophils with EC50values in the nanomolar range[3].
PD 168368 (PD168368) suppresses migration and invasion of the human breast cancer cell line MDA-MB-231. PD 168368 reduces epithelial-mesenchymal transition (EMT) of breast cancer cells by E-cadherin upregulation and vimentin downregulation. PD 168368 (5 μM) inhibits migration and invasiveness in breast cancer cells[4].
PD 168368 (10 μM) suppresses the activation of mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells[4].

Cell Viability Assay[4]

Cell Line:Human breast cancer cell line MDA-MB-231
Concentration:5 μM
Incubation Time:24 hours
Result:Clearly decreased the migratory ability of MDA-MB-231 cells in a Boyden chamber migration assay.

Cell Viability Assay[4]

Cell Line:MDA-MB-231 cells
Concentration:10 μM
Incubation Time:0, 0.5, 1, 2, 4, 8, and 16 hours
Result:Decreased phosphorylation levels of mTOR, p70S6K, 4EBP1, AKT and GSK-3β in a time-dependent manner.
体内研究
(In Vivo)

PD 168368 (PD168368) potently inhibits in vivo metastasis of breast cancer. PD 168368 (1.2 mg/kg; intraperitoneal injection for 30 days) inhibits metastasis of breast cancer in mice[4].

Animal Model:Female BALB/c-nude mice (age 8-10 weeks) bearing MDA-MB-231 xenograft model[4]
Dosage:1.2 mg/kg
Administration:Intraperitoneal injection for 30 days
Result:No metastatic tumor nodules were observed in lungs of PD 168368-treated mice compared to PEG-injected mice.
分子量

554.64

性状

Solid

Formula

C31H34N6O4

CAS 号

204066-82-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 30 mg/mL(54.09 mM;Need ultrasonic and warming)

DMF : 10 mg/mL(18.03 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8030 mL9.0149 mL18.0297 mL
5 mM0.3606 mL1.8030 mL3.6059 mL
10 mM0.1803 mL0.9015 mL1.8030 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。