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Golidocitinib (Synonyms: AZD4205)

Name: Golidocitinib
Brand: TargetMol
SKU: T10431
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

Catalog No. T10431 Copy Product Info

Purity: 99.88%

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Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.

Golidocitinib

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Catalog No. T10431

Synonyms AZD4205

Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.

Cas No. 2091134-68-6

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Pack Size	Price	USA Stock	Global Stock
1 mg	$42	In Stock	In Stock
5 mg	$98	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$259	In Stock	In Stock
50 mg	$396	In Stock	In Stock
100 mg	$645	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$105	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.88%

Appearance:Solid

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.
Targets&IC50	JAK1:73 nM
In vitro	AZD4205 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50: 161 nM).
In vivo	AZD4205, administered orally at doses of 12.5 mg/kg, 25 mg/kg, or 50 mg/kg twice daily (BID), exhibits dose-dependent antitumor effects when used alone. Additionally, it boosts the antitumor efficacy of osimertinib when compared to the administration of osimertinib alone in mice implanted with NCI-H1975 cells.
Synonyms	AZD4205

Chemical Properties

Molecular Weight	489.57
Formula	C₂₅H₃₁N₉O₂
Cas No.	2091134-68-6
Smiles	COc1nn(C)cc1Nc1nccc(n1)-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)CC3)cccc12
Relative Density.	1.38 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (510.65 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.21 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0426 mL	10.2130 mL	20.4261 mL	102.1304 mL
5 mM	0.4085 mL	2.0426 mL	4.0852 mL	20.4261 mL
10 mM	0.2043 mL	1.0213 mL	2.0426 mL	10.2130 mL
20 mM	0.1021 mL	0.5107 mL	1.0213 mL	5.1065 mL
50 mM	0.0409 mL	0.2043 mL	0.4085 mL	2.0426 mL
100 mM	0.0204 mL	0.1021 mL	0.2043 mL	1.0213 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc