Pelitrexol AG 2037|cas:446022-33-9|西域试剂

Pelitrexol AG 2037,98.94%

产品编号：Bellancom-14530| CAS NO：446022-33-9| 分子式：C₂₀H₂₅N₅O₆S| 分子量：463.51

Pelitrexol (AG 2037) 是甘氨酰胺核糖核苷酸甲酰转移酶 ((GARFT)) 的抑制剂。

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-14530	￥5800.00	杭州北京（现货）
Bellancom-14530	￥8800.00	杭州北京（现货）
Bellancom-14530	￥25000.00	杭州北京（现货）
Bellancom-14530	￥40000.00	杭州北京（现货）

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Pelitrexol AG 2037

产品介绍

Pelitrexol (AG 2037) 是甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT) 的抑制剂。Pelitrexol 还通过降低 GTP 结合的 Rheb (mTORC1 专性激活剂) 水平来抑制 mTORC1。Pelitrexol 在小鼠模型中显示出强大的肿瘤生长抑制作用。

生物活性

Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice.

体外研究

Pelitrexo (150 nM; 24 h) profoundly inhibits mTORC1 activity by reducing intracellular guanine nucleotides level as well as GTP-bound Rheb protein level in A549 cells.
Pelitrexo (0-1000 mM; 16 h) strongly inhibits the phosphorylation level of ribosomal protein S6 (S6RP), S6K1, and Chk1 in a dose-dependent manner in NCI-H460 cells.
Pelitrexo (100 nM; 48 h) arrests cell cycle at G1 phase in NCI-H460 cells.

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

Cell Cycle Analysis

Cell Line:	NCI-H460 NSCLC
Concentration:	100 nM
Incubation Time:	4, 8, 24, 48 hours
Result:	Resulted 63% cells accumulation in G1 phase of the cell cycle.

Cell Cycle Analysis

Cell Line:	NCI-H460 NSCLC
Concentration:	0, 10, 30, 100, 300, 1000 nM
Incubation Time:	16 hours
Result:	Inhibits the level of p-S6RP, p-S6K1, and p-Chk1.

体内研究
(In Vivo)

Pelitrexo (10 mg/kg, 20 mg/kg; i.p.; every 4 days for 3 weeks) provokes both mTORC1 inhibition and robust tumor growth suppression in mice bearing nonsmall-cell lung cancer (NSCLC) xenografts.
Pelitrexo (20 mg/kg; i.p.; every 4 days for 3 weeks) inhibits GARFT-dependent purine biosynthesis and blocks mTORC1 function.

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

Animal Model:	Xenograft model of nonsmall-cell lung cancer (NSCLC) in mice
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Intraperitoneal injection; every 4 days for 3 weeks for group 1; administrated at 1, 4, 7 days for group 2
Result:	Inhibited tumor growth by 64% and 69% at 10 mg/kg and 20 mg/kg, respectively in group 1. Inhibited mTORC1-dependent phosphorylation of S6K1, S6RP and CAD at 20 mg/kg in group 2.

体内研究

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

Animal Model:	Xenograft model of nonsmall-cell lung cancer (NSCLC) in mice
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Intraperitoneal injection; every 4 days for 3 weeks for group 1; administrated at 1, 4, 7 days for group 2
Result:	Inhibited tumor growth by 64% and 69% at 10 mg/kg and 20 mg/kg, respectively in group 1. Inhibited mTORC1-dependent phosphorylation of S6K1, S6RP and CAD at 20 mg/kg in group 2.

体内研究

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

Animal Model:	Xenograft model of nonsmall-cell lung cancer (NSCLC) in mice
Dosage:	10 mg/kg, 20 mg/kg
Administration:	Intraperitoneal injection; every 4 days for 3 weeks for group 1; administrated at 1, 4, 7 days for group 2
Result:	Inhibited tumor growth by 64% and 69% at 10 mg/kg and 20 mg/kg, respectively in group 1. Inhibited mTORC1-dependent phosphorylation of S6K1, S6RP and CAD at 20 mg/kg in group 2.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (53.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1575 mL	10.7873 mL	21.5745 mL
5 mM	0.4315 mL	2.1575 mL	4.3149 mL
10 mM	0.2157 mL	1.0787 mL	2.1575 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: ≥ 2.08 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.49 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

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

. Emmanuel N, et al. Purine Nucleotide Availability Regulates mTORC1 Activity through the Rheb GTPase. Cell Rep. 2017 Jun 27;19(13):2665-2680. [Content Brief]

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Pelitrexol AG 2037,98.94%

Pelitrexol AG 2037

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