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. |
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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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 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 | 1 mM | 1.8030 mL | 9.0149 mL | 18.0297 mL | | 5 mM | 0.3606 mL | 1.8030 mL | 3.6059 mL | | 10 mM | 0.1803 mL | 0.9015 mL | 1.8030 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。 |
