GSK621|cas:1346607-05-3|西域试剂

GSK621,98.02%

产品编号：Bellancom-100548| CAS NO：1346607-05-3| 分子式：C₂₆H₂₀ClN₃O₅| 分子量：489.91

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货号	价格	库存与货期
Bellancom-100548	￥1350.00	杭州北京（现货）
Bellancom-100548	￥2300.00	杭州北京（现货）
Bellancom-100548	￥4500.00	杭州北京（现货）

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GSK621

产品介绍

GSK621 是特异性的 AMPK 激动剂，其对 AML 细胞系的IC₅₀ 值为13-30 μM。GSK621 可诱导自噬和凋亡。GSK621 可诱导eiF2α 磷酸化 (UPR 激活的一个标志)。

生物活性

GSK621 is a specific AMPK activator, with IC₅₀ values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.

体外研究

GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation.
GSK621 (30 μM) induces autophagy and apoptosis.
GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells.

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

Cell Proliferation Assay

Cell Line:	MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 AML cell lines. 0-30 μM.
Concentration:	0-30 μM.
Incubation Time:	4 d.
Result:	IC₅₀ values ranged from 13 to 30 μM. Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines.

Cell Autophagy Assay.

Cell Line:	AML cell lines and primary AML samples.
Concentration:	30 μM.
Incubation Time:	24 h.
Result:	Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes.

体内研究
(In Vivo)

GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft.

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

Animal Model:	MOLM-14 cells xenografted into nude mice.
Dosage:	30 mg/kg.
Administration:	IP twice daily.
Result:	Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily.

体内研究

GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft.

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

Animal Model:	MOLM-14 cells xenografted into nude mice.
Dosage:	30 mg/kg.
Administration:	IP twice daily.
Result:	Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily.

体内研究

GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft.

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

Animal Model:	MOLM-14 cells xenografted into nude mice.
Dosage:	30 mg/kg.
Administration:	IP twice daily.
Result:	Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily.

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (25.51 mM; ultrasonic and adjust pH to 1 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0412 mL	10.2060 mL	20.4119 mL
5 mM	0.4082 mL	2.0412 mL	4.0824 mL
10 mM	0.2041 mL	1.0206 mL	2.0412 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： 50% PEG300 50% saline
Solubility: 10 mg/mL (20.41 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 1.25 mg/mL (2.55 mM); Suspended solution; Need ultrasonic

此方案可获得 1.25 mg/mL (2.55 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 12.5 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (2.55 mM); Suspended solution

此方案可获得 ≥ 1.25 mg/mL (2.55 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 12.5 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.55 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.55 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。