GNF-5837|cas:1033769-28-6|西域试剂

GNF-5837,99.45%

产品编号：Bellancom-13491| CAS NO：1033769-28-6| 分子式：C₂₈H₂₁F₄N₅O₂| 分子量：535.49

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-13491	￥500.00	杭州北京（现货）
Bellancom-13491	￥900.00	杭州北京（现货）
Bellancom-13491	￥1500.00	杭州北京（现货）
Bellancom-13491	￥2400.00	杭州北京（现货）
Bellancom-13491	￥4000.00	杭州北京（现货）

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GNF-5837

产品介绍

GNF-5837 是一种有效的，选择性的，口服生物利用的泛 TRK 抑制剂，在 Ba/F3 细胞中显示出抗增殖作用 (对 Tel-TrkC, Tel-TrkB 和 Tel-TrkA 的 IC₅₀ 值分别为 7 nM，9 nM 和 11 nM)。 .

生物活性

GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC₅₀ values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .

体外研究

GNF-5837 (0.1-500 nM; 72-144 hours; GOT1 cells) treatment decreases cell viability in a time- and dose-dependent manner in GOT1 cells.
GNF-5837 (5-500 nM; 24 hours; GOT1 cells) causes downregulation of PI3K-Akt-mTOR signaling, Ras-Raf-MEK-ERK signaling.
GNF-5837 (5-500 nM; 72 hours; GOT1 cells) treatment induces G1 cell cycle arrest.
GNF-5837 (500 nM; 144 hours; GOT1 cells) treatment increases apoptotic cell death.

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

Cell Viability Assay

Cell Line:	GOT1 cells
Concentration:	0.1 nM , 0.5 nM , 1 nM , 5 nM , 10 nM , 50 nM , 100 nM and 500 nM
Incubation Time:	72 hours, 96 hours and 144 hours
Result:	Cell viability assay determined a clear decrease of GOT1 cell viability in a time- and dose- dependent manner.

Western Blot Analysis

Cell Line:	GOT1 cells
Concentration:	5 nM, 50 nM and 500 nM
Incubation Time:	24 hours
Result:	Significant levels of TrkA expression, faint TrkC expression and no TrkB expression.

Cell Cycle Analysis

Cell Line:	GOT1 cells
Concentration:	5 nM, 500 nM
Incubation Time:	72 hours
Result:	Induced G1 cell cycle arrest.

Apoptosis Analysis

Cell Line:	GOT1 cells
Concentration:	500 nM
Incubation Time:	144 hours
Result:	Induced apoptosis.

体内研究
(In Vivo)

GNF-5837 (25-100 mg/kg; oral administration; once daily; for 10 days; mice) treatment inhibits tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.

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

Animal Model:	Mouse xenograft model
Dosage:	25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; for 10 days
Result:	72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.

体内研究

GNF-5837 (25-100 mg/kg; oral administration; once daily; for 10 days; mice) treatment inhibits tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.

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

Animal Model:	Mouse xenograft model
Dosage:	25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; for 10 days
Result:	72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.

体内研究

GNF-5837 (25-100 mg/kg; oral administration; once daily; for 10 days; mice) treatment inhibits tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.

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

Animal Model:	Mouse xenograft model
Dosage:	25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; for 10 days
Result:	72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 32 mg/mL (59.76 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8674 mL	9.3372 mL	18.6745 mL
5 mM	0.3735 mL	1.8674 mL	3.7349 mL
10 mM	0.1867 mL	0.9337 mL	1.8674 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 (4.67 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.67 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 (4.67 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.67 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 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