GNF-5837

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GNF-5837  纯度: 99.45%

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)。 .

GNF-5837

GNF-5837 Chemical Structure

CAS No. : 1033769-28-6

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10 mM * 1 mL in DMSO ￥589 In-stock
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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) [1].

IC50 & Target

TrkB

9 nM (IC50)

TrkC

7 nM (IC50)

TrkA

11 nM (IC50)

体外研究
(In Vitro)

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[2].
GNF-5837 (5-500 nM; 24 hours; GOT1 cells) causes downregulation of PI3K-Akt-mTOR signaling, Ras-Raf-MEK-ERK signaling[2].
GNF-5837 (5-500 nM; 72 hours; GOT1 cells) treatment induces G1 cell cycle arrest[2].
GNF-5837 (500 nM; 144 hours; GOT1 cells) treatment increases apoptotic cell death[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

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[2]

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

Apoptosis Analysis[2]

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse xenograft model[1]
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.

分子量

535.49

Formula

C28H21F4N5O2
CAS 号

1033769-28-6
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
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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Albaugh, P. et al. Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models. ACS MEDICINAL CHEMISTRY LETTERS, 2012; 3 (2): 140

    [2]. Aristizabal Prada ET, et al. Tropomyosin receptor kinase: a novel target in screened neuroendocrine tumors. Endocr Relat Cancer. 2018 May;25(5):547-560.

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