PD 168368,98.78%

产品编号:Bellancom-116216| CAS NO:204066-82-0| 分子式:C31H34N6O4| 分子量:554.64

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-116216
1000.00 杭州 北京(现货)
Bellancom-116216
3000.00 杭州 北京(现货)
Bellancom-116216
4800.00 杭州 北京(现货)
Bellancom-116216
9600.00 杭州 北京(现货)

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PD 168368

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 selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively.

体外研究

PD 168368 (PD168368) is highly active and stimulated [Ca2+]I release in human neutrophils with EC50 values in the nanomolar range.
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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
体内研究

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
性状Solid
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 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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
参考文献

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