Sulfopin PIN1-3|cas:2451481-08-4|西域试剂

Sulfopin PIN1-3,99.90%

产品编号：Bellancom-139361| CAS NO：2451481-08-4| 分子式：C₁₁H₂₀ClNO₃S| 分子量：281.80

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-139361	￥1300.00	杭州北京（现货）
Bellancom-139361	￥2000.00	杭州北京（现货）
Bellancom-139361	￥4200.00	杭州北京（现货）
Bellancom-139361	￥6600.00	杭州北京（现货）
Bellancom-139361	￥10500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Sulfopin PIN1-3

产品介绍

Sulfopin 是一种高选择性共价 Pin1 抑制剂，表观 K_i 值为 17 nM。Sulfopin 在体内阻断 Myc 驱动的肿瘤。肽基脯氨酰异构酶 Pin1 在癌症中被用来激活癌基因和灭活肿瘤抑制因子。

生物活性

Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent K_i of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors.

体外研究

MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days).
Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription.
Sulfopin (1, 2.5 μM; PATU-8988T cells; 4 days) shows a small but significant reduction in the number of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells.

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

Cell Proliferation Assay

Cell Line:	Kuramochi, MDA-MB-468, NGP, NBL-S, MDA-MB-468 cells
Concentration:	1, 2.5 μM
Incubation Time:	4,6, 8 days
Result:	Showed variation in antiproliferative effects across cancer cell lines Kuramochi, MDA-MB-468, NGP and NBL-S, with the most pronounced sensitivity observed in MDA-MB-468 cells.

体内研究
(In Vivo)

Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice.
Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice.
Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish.

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

Animal Model:	Transgenic Th-MYCN mice
Dosage:	40 mg/kg
Administration:	Once a day (QD) or twice a day (BID) for 7 days
Result:	Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.

体内研究

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

Animal Model:	Transgenic Th-MYCN mice
Dosage:	40 mg/kg
Administration:	Once a day (QD) or twice a day (BID) for 7 days
Result:	Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.

体内研究

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

Animal Model:	Transgenic Th-MYCN mice
Dosage:	40 mg/kg
Administration:	Once a day (QD) or twice a day (BID) for 7 days
Result:	Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (354.86 mM; Need ultrasonic)

H₂O : 4.35 mg/mL (15.44 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5486 mL	17.7431 mL	35.4862 mL
5 mM	0.7097 mL	3.5486 mL	7.0972 mL
10 mM	0.3549 mL	1.7743 mL	3.5486 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 (8.87 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.87 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.87 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.87 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.87 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.87 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。