GNE-617

Name: GNE-617
Brand: MedChemExpress
SKU: HY-15766
Rating: 5.0 (7 reviews)

製品番号: HY-15766 純度: 99.58%: Data Sheet SDS COA 取扱説明書
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GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

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CAS 番号 : 1362154-70-8

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 108	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 108	在庫あり	Estimated Time of Arrival: December 31
Solid
2 mg	$61	在庫あり	Estimated Time of Arrival: December 31
5 mg	$99	在庫あり	Estimated Time of Arrival: December 31
10 mg	$165	在庫あり	Estimated Time of Arrival: December 31
25 mg	$330	在庫あり	Estimated Time of Arrival: December 31
50 mg	$495	在庫あり	Estimated Time of Arrival: December 31
100 mg	$825	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

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* アイテムを追加する前、数量をご選択ください

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Based on 7 publication(s) in Google Scholar

Other Forms of GNE-617:

GNE-617 hydrochloride 在庫あり
GNE-617 (Standard) お問い合わせ

顧客検証

•Oncotarget. 2018 Mar 27;9(23):16451-16461. [Abstract]

Cell Proliferation/Viability Assay

: GNE-617 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Mar 27;9(23):16451-16461. [Abstract]; Drug sensitivities of HCT116R^FK866 and HCT116 in the colony formation assay. HCT116R^FK866 and HCT116 cells are treated with 100 nM each of FK866, CHS-828, GNE-617, STF-118804, and incubated for 10 days.

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製品説明

GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

IC₅₀ & Target

IC50: 5 nM (NAMPT)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.002 μM Compound: 1; GNE-617	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	[PMID: 27541271]
A2780	IC₅₀	0.002 μM Compound: 58	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis	[PMID: 23859118]
B16-F10	IC₅₀	71 nM Compound: 4	Antiproliferative activity against mouse B16F10 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against mouse B16F10 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
COS-1	IC₅₀	5 nM Compound: 4	Cytotoxicity against African green monkey COS1 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Cytotoxicity against African green monkey COS1 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
COS-7	IC₅₀	9 nM Compound: 4	Cytotoxicity against African green monkey COS7 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Cytotoxicity against African green monkey COS7 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
Calu-6	IC₅₀	5 nM Compound: 4	Antiproliferative activity against human Calu6 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human Calu6 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
HCT-116	IC₅₀	2 nM Compound: 4	Antiproliferative activity against human HCT116 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human HCT116 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
HCT-116	IC₅₀	2 nM Compound: 58	Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
HT-1080	IC₅₀	2 nM Compound: 4	Antiproliferative activity against human HT1080 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human HT1080 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
HT-1080	IC₅₀	2.1 nM Compound: 58	Antiproliferative activity against human HT1080 cells assessed as cell viability after 72 hrs Antiproliferative activity against human HT1080 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
MIA PaCa-2	IC₅₀	7 nM Compound: 4	Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
MIA PaCa-2	IC₅₀	7.4 nM Compound: 58	Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 72 hrs Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
PC-3	EC₅₀	1.1 nM Compound: 4	Inhibition of NAMPT in human PC3 cells assessed as reduction in NAD level after 48 hrs by mass spectrometry Inhibition of NAMPT in human PC3 cells assessed as reduction in NAD level after 48 hrs by mass spectrometry	[PMID: 24021463]
PC-3	IC₅₀	2.7 nM Compound: 58	Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs	[PMID: 23859118]
PC-3	IC₅₀	3 nM Compound: 4	Antiproliferative activity against human PC3 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Antiproliferative activity against human PC3 cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
RF/6A	IC₅₀	4 nM Compound: 4	Cytotoxicity against rhesus monkey RF/6A cells assessed as cell viability after 96 hrs by CyQuant staining-based assay Cytotoxicity against rhesus monkey RF/6A cells assessed as cell viability after 96 hrs by CyQuant staining-based assay	[PMID: 24021463]
U-251	IC₅₀	1.8 nM Compound: 58	Antiproliferative activity against human U251 cells assessed as cell viability after 72 hrs by SRB assay Antiproliferative activity against human U251 cells assessed as cell viability after 72 hrs by SRB assay	[PMID: 23859118]

体外実験

The activity ofGNE-617 hydrochloride is evaluated on a panel 53 non-small cell lung cancer (NSCLC) cell lines in the presence or absence of 10 μM nicotinic acid. GNE-617 inhibits NAMPT IC50 of 18.9 nM in A549 cell.The majority of cell lines exhibit a steep dose response to GNE-617 when evaluated by decrease in ATP or total nucleic acid, and the cytotoxicity is completely rescued by simultaneous addition of nicotinic acid. The majority of the cell lines tested have IC₅₀ values below 100 nM, with approximately half with IC₅₀ values less than 10 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

In rats, GNE-617 (administered QD) and GNE-875 (administered BID) are associated with more severe retinal toxicity at similar exposures and dosing duration compared with GMX-1778 (administered BID). The mouse efficacy studies using GNE-617, GNE-618, and GMX-1778 are designed to assess efficacy and opportunistically used to assess retinal toxicity in mice. NAMPTi retinal toxicity is observed with GNE-617 and GMX-1778; however, the different study durations between GNE-617 and GMX-1778 do not allow for direct comparison of retinal toxicity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

427.42

分子式

C₂₁H₁₅F₂N₃O₃S

CAS 番号

1362154-70-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=C(S(C2=CC(F)=CC(F)=C2)(=O)=O)C=C1)C3=CN4C(C=C3)=NC=C4

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 : 16.67 mg/mL (39.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3396 mL	11.6981 mL	23.3962 mL
5 mM	0.4679 mL	2.3396 mL	4.6792 mL
10 mM	0.2340 mL	1.1698 mL	2.3396 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: ≥ 1.67 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.58%

Select Batch:

データシート (279 KB) SDS (393 KB)

COA (246 KB) LCMS (95 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23. [Content Brief]

[2]. Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72. [Content Brief]

キナーゼ実験 ^[1]	For RNA interference (RNAi), A549 cells are plated at 1,500 cells per well in 96-well plates, allowed to adhere for 24 hours, and transfected with 25 nM siRNA oligonucleotide using Dharmafect 4. Transfected cells are treated with the indicated concentrations of GNE-617 (0.1, 1 , 10 , 100 , and 1000 nM) for 72 hours and viability is evaluated with CellTiter-Glo. Lysates for detection of NAPRT1 protein are collected 72 hours after transfection of 1 million A549 cells in 10 cm dishes. For NAPRT1 re-expression, RERF-LC-MS cells are transfected with pCMV6-AC.NAPRT1 and empty vector pCMV6-AC using Amaxa Nucleofector technology and selected with Geneticin^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
細胞実験 ^[1]	Cells are grown in RPMI-1640 medium supplemented with 10% FBS and 2 mM glutamine and passaged not more than 20 times after thawing. To determine the IC₅₀ values and nicotinic acid rescue status, cells are treated with nine point dose titrations of GNE-617 with or without 10 μM nicotinic acid. At 96 hours post-drug addition, the GNE-617-treated cells are evaluated using CyQUANT Direct Cell Proliferation Assay followed by CellTiter-Glo Luminescent Cell Viability Assay quantified with a Wallac EnVision 2104 Multilabel Reader. IC₅₀ values are calculated using XLfit 5.1. To examine the protein level, cells are lysed in ice-cold radioimmunoprecipitation assay buffer, run on SDS-PAGE (4%-12% Bis-Tris), and evaluated by Western blotting using antibodies directed against NAPRT1 and β-actin^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[2]	Rats^[2] Male naïve Sprague Dawley rats are administered once daily (QD) via oral gavage either (1) GNE-617 at 30 mg/kg for 2 consecutive days in combination with NA at 75 mg/kg twice daily (BID; 6 h apart); (2) GNE-618 at 30 mg/kg for 1 day; or (3) GMX-1778 at 30 mg/kg for 1 day. Dose selection for each compound is based on tolerability and toxicity findings from the safety studies and for nicotinic acid (NA) on the highest concentration of NA that could be administered to rats in a solution form. Formulating NA at higher concentration resulted in a suspension, and NA is determined to be unstable in a suspension form. GNE-617, GNE-618, and GMX-1778 are formulated as a solution in the vehicle of 60% polyethylene glycol (PEG 400)/10% ethanol/30% 5% dextrose in water (D5W) (vol/vol/vol), and NA is formulated as a solution in water. At 1 h and 6.5 h post-dose (on Day 2 for GNE-617), rats (3-4 rats per time point) are euthanized, and the blood, retina, and brain are collected. Blood samples are collected into K₂EDTA Microtainer tubes. The tubes are chilled on wet ice until centrifugation within 30 min of collection. Plasma is collected and transferred to 1.2 mL cluster tubes. Tissues are rinsed with phosphate-buffered saline and blotted dry using gauze. All samples are stored at more than −80°C until compound analysis. Results are expressed as an absolute concentration in retina, brain, or plasma and as a ratio of retina:plasma concentration. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Shames DS, et al. Loss of NAPRT1 Expression by Tumor-specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT Inhibitors. Clin Cancer Res. 2013 Dec 15;19(24):6912-23. [Content Brief] [2]. Zabka TS, et al. Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase. Toxicol Sci. 2015 Mar;144(1):163-72. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.3396 mL	11.6981 mL	23.3962 mL	58.4905 mL
	5 mM	0.4679 mL	2.3396 mL	4.6792 mL	11.6981 mL
	10 mM	0.2340 mL	1.1698 mL	2.3396 mL	5.8490 mL
	15 mM	0.1560 mL	0.7799 mL	1.5597 mL	3.8994 mL
	20 mM	0.1170 mL	0.5849 mL	1.1698 mL	2.9245 mL
	25 mM	0.0936 mL	0.4679 mL	0.9358 mL	2.3396 mL
	30 mM	0.0780 mL	0.3899 mL	0.7799 mL	1.9497 mL

GNE-617 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:

GNE-6171362154-70-8GNE617GNE 617NAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorInhibitorinhibitorinhibit

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GNE-617

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Other Forms of GNE-617:

GNE-617 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

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•関連タンパク質:

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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

GNE-617 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GNE-617 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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