Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

GSK3145095 [1622849-43-7]

Stampa

Cat# HY-111946-1ml

Size : 10mM/1mL

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Telefono : +1 850 650 7790

Marca : MedChemExpress

Contatta il distributore locale :

Telefono : +1 850 650 7790

GSK3145095 is a RIP1 kinase inhibitor with an IC₅₀ of 6.3 nM .

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GSK3145095 Chemical Structure

CAS No. : 1622849-43-7

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

Based on 1 publication(s) in Google Scholar

Description

GSK3145095 is a RIP1 kinase inhibitor with an IC₅₀ of 6.3 nM ^[1].

IC₅₀ & Target

IC50: 6.3 nM (RIP1 kinase )^[1]

In Vitro

GSK3145095 potently blocks the TNF response as shown by determination of overall cell viability as measured by cellular ATP levels (IC₅₀ = 1.6 nM), cell death as measured by LDH release (IC₅₀ = 0.5 nM) and RIP1-dependent inflammatory cytokine MIP-1β production, either as absolute levels for protein, or fold changes in mRNA expression (IC₅₀ = 0.4 nM) ^[1].

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

Essai clinique

Masse moléculaire

397.38

Formule

C₂₀H₁₇F₂N₅O₂

CAS No.

1622849-43-7

Appearance

Solid

Color

White to off-white

SMILES

FC1=CC(F)=CC2=C1NC([C@@H](NC(C3=NNC(CC4=CC=CC=C4)=N3)=O)CC2)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (629.12 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	2.5165 mL	12.5824 mL	25.1648 mL
5 mM	0.5033 mL	2.5165 mL	5.0330 mL
10 mM	0.2516 mL	1.2582 mL	2.5165 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.

Calculateur de molarité
Calculateur de dilution

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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: ≥ 2.08 mg/mL (5.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

Pureté et documentation

Purity: 99.39%

Select Batch:

Fiche technique (273 KB) SDS (252 KB)

COA (249 KB) LCMS (266 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Harris PA, ET AL. Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer. ACS Med Chem Lett. 2019 May 9;10(6):857-862. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5165 mL	12.5824 mL	25.1648 mL	62.9121 mL
	5 mM	0.5033 mL	2.5165 mL	5.0330 mL	12.5824 mL
	10 mM	0.2516 mL	1.2582 mL	2.5165 mL	6.2912 mL
	15 mM	0.1678 mL	0.8388 mL	1.6777 mL	4.1941 mL
	20 mM	0.1258 mL	0.6291 mL	1.2582 mL	3.1456 mL
	25 mM	0.1007 mL	0.5033 mL	1.0066 mL	2.5165 mL
	30 mM	0.0839 mL	0.4194 mL	0.8388 mL	2.0971 mL
	40 mM	0.0629 mL	0.3146 mL	0.6291 mL	1.5728 mL
	50 mM	0.0503 mL	0.2516 mL	0.5033 mL	1.2582 mL
	60 mM	0.0419 mL	0.2097 mL	0.4194 mL	1.0485 mL
	80 mM	0.0315 mL	0.1573 mL	0.3146 mL	0.7864 mL
	100 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6291 mL

GSK3145095 [1622849-43-7]

Cat# HY-111946-1ml

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

GSK3145095 Related Classifications

Keywords:

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GSK3145095 [1622849-43-7]

Cat# HY-111946-1ml

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

GSK3145095 Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

GSK3145095 Related Classifications

Keywords:

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