GSK547 GSK'547|cas:2226735-55-1|西域试剂

GSK547 GSK'547,99.84%

产品编号：Bellancom-114492| CAS NO：2226735-55-1| 分子式：C₂₀H₁₈F₂N₆O| 分子量：396.39

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货号	价格	库存与货期
Bellancom-114492	￥1500.00	杭州北京（现货）
Bellancom-114492	￥2550.00	杭州北京（现货）
Bellancom-114492	￥5100.00	杭州北京（现货）
Bellancom-114492	￥8500.00	杭州北京（现货）
Bellancom-114492	￥13500.00	杭州北京（现货）

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GSK547 GSK'547

产品介绍

GSK547 (GSK'547) 是一种高效的选择性 receptor-interacting serine/threonine protein kinase 1 (RIPK1) 抑制剂，可抑制巨噬细胞介导的胰腺癌适应性免疫耐受。

生物活性

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.

体外研究

GSK547 (0.1-100000 nM; 24 hours) pretreats L929 cells with recombinant TNFα and zVAD at various doses for 30 min, then cell death is induced with an IC₅₀ of 32 nM after 24 hours.
GSK547 up-regulates STAT1 signaling in bone marrow-derived macrophages (BMDM).

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

Cell Viability Assay

Cell Line:	L929 cells (Mouse L-cells NCTC 929)
Concentration:	0.1 nM; 10 nM; 1000 nM; 100000 nM
Incubation Time:	24 hours
Result:	Reduced viability of L929 cells after co-treatment with TNFα and zVAD with an IC₅₀ of 32 nM.

Western Blot Analysis

Cell Line:	Bone marrow-derived macrophages (BMDM)
Concentration:
Incubation Time:	30 minutes
Result:	Up-regulated STAT1 signaling in BMDM.

体内研究
(In Vivo)

GSK547 (GSK′547; RIP1i) robustly targets RIP1 in vivo. RIP1 inhibition results in immunogenic macrophage differentiation in pancreatic cancer, leading to adaptive immune activation and tumor protection for pancreatic ductal adenocarcinoma (PDA).
GSK547 (100 mg/kg/day; fed via food-based dosing; 15-50 days) reduces tumor burden and extends survival compared with mice treated with controls or Nec-1s.

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

Animal Model:	The wild-type (WT) mice orthotopically implanted with Pdx1^Cre;Kras^G12D;Trp53^R172H (KPC)-derived tumor cells
Dosage:	~100 mg/kg
Administration:	Fed via food-based dosing, daily, 15-50 days
Result:	Reduced tumor burden and extended survival.

体内研究

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

Animal Model:	The wild-type (WT) mice orthotopically implanted with Pdx1^Cre;Kras^G12D;Trp53^R172H (KPC)-derived tumor cells
Dosage:	~100 mg/kg
Administration:	Fed via food-based dosing, daily, 15-50 days
Result:	Reduced tumor burden and extended survival.

体内研究

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

Animal Model:	The wild-type (WT) mice orthotopically implanted with Pdx1^Cre;Kras^G12D;Trp53^R172H (KPC)-derived tumor cells
Dosage:	~100 mg/kg
Administration:	Fed via food-based dosing, daily, 15-50 days
Result:	Reduced tumor burden and extended survival.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (630.69 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5228 mL	12.6138 mL	25.2277 mL
5 mM	0.5046 mL	2.5228 mL	5.0455 mL
10 mM	0.2523 mL	1.2614 mL	2.5228 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 (stored under nitrogen)。-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： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.25 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。