PACMA 31|cas:1401089-31-3|西域试剂

PACMA 31,99.75%

产品编号：Bellancom-100433| CAS NO：1401089-31-3| 分子式：C₂₁H₂₂N₂O₆S| 分子量：430.47

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100433	￥1200.00	杭州北京（现货）
Bellancom-100433	￥2000.00	杭州北京（现货）
Bellancom-100433	￥4400.00	杭州北京（现货）
Bellancom-100433	￥7300.00	杭州北京（现货）
Bellancom-100433	￥11700.00	杭州北京（现货）

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PACMA 31

产品介绍

PACMA 31 是一种不可逆的口服活性蛋白二硫化物异构酶 (PDI) 抑制剂，IC₅₀ 为 10μM，PACMA 31与 PDI 的活性部位半胱氨酸形成共价键。PACMA 31 具有肿瘤靶向性，能显著抑制卵巢肿瘤生长，对正常组织无毒性。

生物活性

PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC₅₀ of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.

体外研究

PACMA 31 (0-10 μM; 24 hours) significantly inhibits colony formation in OVCAR-8 cells in a dose-dependent manner.

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

体内研究

PACMA 31 (20-200 mg/kg; i.p.; daily for 62 days) suppresses tumor growth in human ovarian cancer mouse xenografts .

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

Animal Model:	Athymic mice (bearing OVCAR-8 cells)
Dosage:	20-200 mg/kg
Administration:	I.p., per day for the first 3 wk with 5-d on and 2-d off treatment cycles, and dose was escalated to 40 mg/kg per day for the next 7 d; p.o., the initial dose of 20 mg/kg per day was gradually increased by 20 mg/kg per day with each dose for 3 d before it was orally dosed at 200 mg/kg per day for an additional 32 d, increasing the dose from 20 to 200 mg/kg
Result:	Compared with the control group, i.p. or per os administration of PACMA 31 significantly inhibited tumor growth by 85% and 65% at day 62, respectively.

体内研究

PACMA 31 (20-200 mg/kg; i.p.; daily for 62 days) suppresses tumor growth in human ovarian cancer mouse xenografts .

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

Animal Model:	Athymic mice (bearing OVCAR-8 cells)
Dosage:	20-200 mg/kg
Administration:	I.p., per day for the first 3 wk with 5-d on and 2-d off treatment cycles, and dose was escalated to 40 mg/kg per day for the next 7 d; p.o., the initial dose of 20 mg/kg per day was gradually increased by 20 mg/kg per day with each dose for 3 d before it was orally dosed at 200 mg/kg per day for an additional 32 d, increasing the dose from 20 to 200 mg/kg
Result:	Compared with the control group, i.p. or per os administration of PACMA 31 significantly inhibited tumor growth by 85% and 65% at day 62, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (232.30 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3230 mL	11.6152 mL	23.2304 mL
5 mM	0.4646 mL	2.3230 mL	4.6461 mL
10 mM	0.2323 mL	1.1615 mL	2.3230 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 (5.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.81 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 (5.81 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.81 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。