PR-924|cas:1416709-79-9|西域试剂

PR-924,99.34%

产品编号：Bellancom-123587| CAS NO：1416709-79-9| 分子式：C₃₇H₃₈N₄O₅| 分子量：618.72

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-123587		￥5500.00	杭州北京（现货）
Bellancom-123587		￥8800.00	杭州北京（现货）

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PR-924

产品介绍

PR-924 是一种选择性三肽环氧酮免疫蛋白酶亚单位 LMP-7 的抑制剂，IC₅₀ 为 22 nM。PR-924 共价修饰蛋白酶体的 N 端苏氨酸活性位点。PR-924 在多发性骨髓瘤细胞中抑制细胞生长并触发凋亡 (apoptosis)，并具有抗肿瘤活性。

生物活性

PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC₅₀ of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities.

体外研究

PR-924 (1-20 μM; 24-72 hours; MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells) treatment significantly decreases the viability of all the MM cell lines in a time-and dose-dependent manner (IC ₅₀ range for cell lines: 3-7 μM for 48 h).
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells.
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein, without altering Bax or MCL-1 protein levels.
PR-924 induces BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondria-mediated apoptotic signaling pathways via cyto-c release.

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

Cell Viability Assay

Cell Line:	MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells
Concentration:	1-20 μM
Incubation Time:	24 hours, 48 hours, and 72 hours
Result:	Significantly decreased the viability of all the MM cell lines in a time-and dose-dependent manner (IC ₅₀ range for cell lines: 3-7 μM for 48 h).

Apoptosis Analysis

Cell Line:	MM.1S and MM.1R cells
Concentration:	3 μM
Incubation Time:	48 hours
Result:	Triggered a significant increase in the Annexin V+/PI-apoptotic cell population.

Western Blot Analysis

Cell Line:	MM.1S and MM.1R cells
Concentration:	3 μM
Incubation Time:	48 hours
Result:	Triggered activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein.

体内研究
(In Vivo)

PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment significantly inhibits tumour growth in human plasmacytoma xenografts.
PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival.

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

Animal Model:	CB-17 SCID-mice injected with MM.1S cells
Dosage:	6 mg/kg
Administration:	Intravenous injection; twice a week; for 21 days
Result:	Inhibited tumour growth in human plasmacytoma xenografts.

体内研究

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

Animal Model:	CB-17 SCID-mice injected with MM.1S cells
Dosage:	6 mg/kg
Administration:	Intravenous injection; twice a week; for 21 days
Result:	Inhibited tumour growth in human plasmacytoma xenografts.

体内研究

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

Animal Model:	CB-17 SCID-mice injected with MM.1S cells
Dosage:	6 mg/kg
Administration:	Intravenous injection; twice a week; for 21 days
Result:	Inhibited tumour growth in human plasmacytoma xenografts.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (80.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6162 mL	8.0812 mL	16.1624 mL
5 mM	0.3232 mL	1.6162 mL	3.2325 mL
10 mM	0.1616 mL	0.8081 mL	1.6162 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.04 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.04 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。