GNF-5837

Name: GNF-5837
Brand: MedChemExpress
SKU: HY-13491
Rating: 5.0 (4 reviews)

製品番号: HY-13491 純度: 99.44%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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) .

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

GNF-5837 構造式

CAS 番号 : 1033769-28-6

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 65	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 65	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$55	在庫あり	Estimated Time of Arrival: December 31
10 mg	$99	在庫あり	Estimated Time of Arrival: December 31
25 mg	$165	在庫あり	Estimated Time of Arrival: December 31
50 mg	$264	在庫あり	Estimated Time of Arrival: December 31
100 mg	$440	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

顧客検証

Trk Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

TrkA TrkB TrkC Trk

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

TrkB

9 nM (IC₅₀)

TrkC

7 nM (IC₅₀)

TrkA

11 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A10	IC₅₀	0.5 μM Compound: 22, GNF-5837	Inhibition of PDGFR in rat A10 cells Inhibition of PDGFR in rat A10 cells	[PMID: 24900443]
BaF3	IC₅₀	0.007 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKC Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKC	[PMID: 24900443]
BaF3	IC₅₀	0.009 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKB Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKB	[PMID: 24900443]
BaF3	IC₅₀	0.011 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKA Antiproliferative activity against mouse BA/F3 cells expressing Tel-TRKA	[PMID: 24900443]
BaF3	IC₅₀	0.042 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing TRKA and NGF Antiproliferative activity against mouse BA/F3 cells expressing TRKA and NGF	[PMID: 24900443]
BaF3	IC₅₀	0.87 μM Compound: 22, GNF-5837	Inhibition of Tel-fused PDGFRbeta in mouse BA/F3 cells Inhibition of Tel-fused PDGFRbeta in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	0.91 μM Compound: 22, GNF-5837	Inhibition of Tel-fused KIT in mouse BA/F3 cells Inhibition of Tel-fused KIT in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	2.9 μM Compound: 22, GNF-5837	Inhibition of Tel-fused JNK2 in mouse BA/F3 cells Inhibition of Tel-fused JNK2 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	3 μM Compound: 22, GNF-5837	Antiproliferative activity against mouse BA/F3 cells expressing Tel-KDR Antiproliferative activity against mouse BA/F3 cells expressing Tel-KDR	[PMID: 24900443]
BaF3	IC₅₀	3.4 μM Compound: 22, GNF-5837	Inhibition of Tel-fused ALK in mouse BA/F3 cells Inhibition of Tel-fused ALK in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	3.6 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FGR in mouse BA/F3 cells Inhibition of Tel-fused FGR in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FMS in mouse BA/F3 cells Inhibition of Tel-fused FMS in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4.4 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FLT1 in mouse BA/F3 cells Inhibition of Tel-fused FLT1 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused RON in mouse BA/F3 cells Inhibition of Tel-fused RON in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	4.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused ZAP70 in mouse BA/F3 cells Inhibition of Tel-fused ZAP70 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.1 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FLT3 in mouse BA/F3 cells Inhibition of Tel-fused FLT3 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused RET in mouse BA/F3 cells Inhibition of Tel-fused RET in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.6 μM Compound: 22, GNF-5837	Antiproliferative activity against wild type mouse BA/F3 cells in presence of IL3 Antiproliferative activity against wild type mouse BA/F3 cells in presence of IL3	[PMID: 24900443]
BaF3	IC₅₀	5.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused TIE1 in mouse BA/F3 cells Inhibition of Tel-fused TIE1 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.8 μM Compound: 22, GNF-5837	Inhibition of Tel-fused EPHB2 in mouse BA/F3 cells Inhibition of Tel-fused EPHB2 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.8 μM Compound: 22, GNF-5837	Inhibition of Tel-fused MET in mouse BA/F3 cells Inhibition of Tel-fused MET in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	5.9 μM Compound: 22, GNF-5837	Inhibition of Tel-fused EPHA3 in mouse BA/F3 cells Inhibition of Tel-fused EPHA3 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	6 μM Compound: 22, GNF-5837	Inhibition of Tel-fused ROS in mouse BA/F3 cells Inhibition of Tel-fused ROS in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	6.7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused BMX in mouse BA/F3 cells Inhibition of Tel-fused BMX in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	6.8 μM Compound: 22, GNF-5837	Inhibition of NMP-ALK in mouse BA/F3 cells Inhibition of NMP-ALK in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FGFR4 in mouse BA/F3 cells Inhibition of Tel-fused FGFR4 in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused LYN in mouse BA/F3 cells Inhibition of Tel-fused LYN in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused SRC in mouse BA/F3 cells Inhibition of Tel-fused SRC in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	7.6 μM Compound: 22, GNF-5837	Inhibition of Tel-fused IGF1R in mouse BA/F3 cells Inhibition of Tel-fused IGF1R in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	8 μM Compound: 22, GNF-5837	Inhibition of Tel-fused INSR in mouse BA/F3 cells Inhibition of Tel-fused INSR in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	8.2 μM Compound: 22, GNF-5837	Inhibition of Bcr-ABL in mouse BA/F3 cells Inhibition of Bcr-ABL in mouse BA/F3 cells	[PMID: 24900443]
BaF3	IC₅₀	9.3 μM Compound: 22, GNF-5837	Inhibition of Tel-fused FGFR3 in mouse BA/F3 cells Inhibition of Tel-fused FGFR3 in mouse BA/F3 cells	[PMID: 24900443]

体外実験

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].

MedChemExpress (MCE) 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.

体内実験

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].

MedChemExpress (MCE) 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

分子式

C₂₈H₂₁F₄N₅O₂

CAS 番号

1033769-28-6

Appearance

Solid

Color

Orange to red

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C)C(NC3=CC(NC/4=O)=C(C=C3)C4=C\C5=CC=CN5)=C2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : ≥ 32 mg/mL (59.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.67 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.44%

Select Batch:

データシート (278 KB) SDS (393 KB)

COA (247 KB) HNMR (180 KB) RP-HPLC (244 KB) MS (68 KB)

取扱説明書 (2659 KB)

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 [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8674 mL	9.3372 mL	18.6745 mL	46.6862 mL
	5 mM	0.3735 mL	1.8674 mL	3.7349 mL	9.3372 mL
	10 mM	0.1867 mL	0.9337 mL	1.8674 mL	4.6686 mL
	15 mM	0.1245 mL	0.6225 mL	1.2450 mL	3.1124 mL
	20 mM	0.0934 mL	0.4669 mL	0.9337 mL	2.3343 mL
	25 mM	0.0747 mL	0.3735 mL	0.7470 mL	1.8674 mL
	30 mM	0.0622 mL	0.3112 mL	0.6225 mL	1.5562 mL
	40 mM	0.0467 mL	0.2334 mL	0.4669 mL	1.1672 mL
	50 mM	0.0373 mL	0.1867 mL	0.3735 mL	0.9337 mL

GNF-5837 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNF-58371033769-28-6GNF5837GNF 5837Trk ReceptorTropomyosin related kinase receptorInhibitorinhibitorinhibit

最近チェックした製品:

製品名

カスタマ需要量 *

お名前 *

タイトル

メールアドレス *

電話番号 *

デパートメント

組纖名 *

市区町村

都道府県

国或いは地域 *

必ず会社名を記載ください。個人への返信は行いません。

備考

製品名

Lot #

お名前 *

メールアドレス *

電話番号 *

部門 *

組纖名 *

国或いは地域 *

備考

GNF-5837

カスタマーレビュー

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Trk Receptor アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GNF-5837 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

お名前
メール *

	Sorry, but the email address you supplied was invalid.

GNF-5837

カスタマーレビュー

GNF-5837 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Trk Receptor アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

GNF-5837 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GNF-5837 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report