GANT 58|64048-12-0|(NSC 75503)-陌孚医药/Medlife

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GANT 58 (Synonyms: NSC 75503)

目录号: PC14769 纯度: ≥98%

CAS No. :64048-12-0

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PC14769-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥597.80	请登录

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中文名称

GANT 58

中文别名

2,3,4,5-四-(4-吡啶)噻吩;2,3,4,5-四(4-吡啶基)噻吩;4,4?4乔,4乔?(2,3,4,5-Thiophentetrayl)tetrakis-pyridine

英文名称

GANT 58

英文别名

Pyridine,4,4',4'',4'''-(2,3,4,5-thiophenetetrayl)tetrakis-;(2,3,4,5-THIOPHENTETRAYL)TETRAKIS-PYRIDINE;4-(2,4,5-tripyridin-4-ylthiophen-3-yl)pyridine;GANT 58;4,4',4'',4'''-thiophenetetrayl-tetra-pyridine;4,4',4'',4'''-Thiophentetrayl-tetra-pyridin;GANT-58;NSC 75503;NSC-75503;tetra-<4-pyridyl>thiophene;2,3,4,5-Tetra(4-pyridyl)thiophene;4,4′,4′′,4′′′-Thiene-2,3,4,5-tetrayltetrapyridine;1,2,3,4-Tetrakis(4-pyridyl)thiophene;4,4',4'',4'''-(2,3,4,5-Thiophenetetrayl)tetrakispyridine;2,3,4,5-Tetra-(4-Pyridyl) Thiophene

Cas No.

64048-12-0

分子式

C₂₄H₁₆N₄S

分子量

392.48

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

GANT 58 (NSC 75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with IC₅₀ of 5 μM.

性状

Solid

IC50 & Target[1][2]

IC50: 5 μM (Gli)

体外研究(In Vitro)

GANT58 is a downstream inhibitor of Hh signaling. GANT58 is an indeed inhibitor of Hh signaling downstream of Smo and Sufu. GANT58 mainly acts at the nuclear level because transcription induced by GLI1 with a mutated nuclear export signal is still blocked. GANT58 efficiently inhibits 体外研究 tumor cell proliferation in a GLI-dependent manner and successfully blocks cell growth using human prostate cancer cells harboring downstream activation of the Hh pathway. GANT58 (NSC75503) has been shown to inhibit transcriptional activation by GLI1 (as well as by the other GLI species). GANT58 has been shown to inhibit GLI transactivation.

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

体内研究(In Vivo)

Nude mice are injected s.c. with GLI1-positive 22Rv1 prostate cancer cells, and tumors are established (median size ≈250 mm). Nude mice are treated with daily s.c. injections at a concentration of 50 mg/kg of cyclopamine, GANT61, GANT58, or solvent only (n=4-5 for each group). However, after 3 days, cyclopamine-treated animals presented with severe ulcerations at the injection sites. Therefore, changing the treatment regimen to injections only every second day. To be able to compare all compounds, this protocol is also introduced for the GANTs, although mice treated with these compounds showed no such signs of toxicity. All injections are done 2-3 cm away from the tumors. During an 18-day treatment period, suppression of tumor cell growth is observed for all compounds. Treatment with cyclopamine or GANT58 results in the inhibition of additional xenograft growth and limited the increase in tumor size.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. [Information]

[2]. Joo J, et al. GLI1 is a central mediator of EWS/FLI1 signaling in Ewing tumors. PLoS One. 2009 Oct 27;4(10):e7608. [Information]

溶解度数据

体外研究:

Ethanol : 20 mg/mL (50.96 mM; Need ultrasonic)

DMSO : 9.09 mg/mL (23.16 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5479 mL	12.7395 mL	25.4790 mL
5 mM	0.5096 mL	2.5479 mL	5.0958 mL
10 mM	0.2548 mL	1.2740 mL	2.5479 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 45% PEG300 5% Tween-80 50% saline
Solubility: 5 mg/mL (12.74 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic

此方案可获得 2 mg/mL (5.10 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 EtOH 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (5.10 mM); Clear solution; Need ultrasonic

此方案可获得 2 mg/mL (5.10 mM) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 EtOH 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
4.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

此方案可获得 ≥ 0.91 mg/mL (2.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 9.1 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 ddH?O 中，得到澄清透明的生理盐水溶液
5.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

此方案可获得 ≥ 0.91 mg/mL (2.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 9.1 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
6.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 0.91 mg/mL (2.32 mM); Clear solution

此方案可获得 ≥ 0.91 mg/mL (2.32 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 9.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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