Golidocitinib (Synonyms: AZD4205)

Name: Golidocitinib
Brand: MedChemExpress
SKU: HY-107361
Rating: 5.0 (2 reviews)

Cat. No.: HY-107361 Pureza: 99.54%: Ficha de datos
COA

SDS
Instrucciones de manejo
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Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC₅₀ of 73 nM, weakly inhibits JAK2 (IC₅₀>14.7 μM), and shows little inhibition on JAK3 (IC₅₀>30 μM).

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Golidocitinib Estructura química

No. CAS : 2091134-68-6

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 2 publication(s) in Google Scholar

Other Forms of Golidocitinib:

Golidocitinib (Standard) Obtener un presupuesto

2 Publications Citing Use of MCE Golidocitinib

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas JAK:

Ver todas las isoformas

JAK1 JAK2 JAK3 Tyk2 JAK

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC₅₀ of 73 nM, weakly inhibits JAK2 (IC₅₀>14.7 μM), and shows little inhibition on JAK3 (IC₅₀>30 μM)^[1].

IC₅₀ & Target^[1]

JAK1

73 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1975	IC₅₀	0.13 3 Compound: 21; AZD4205	Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA	[PMID: 32297743]
NCI-H1975	IC₅₀	0.13 3 Compound: 21; AZD4205	Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA	[PMID: 32297743]
NCI-H1975	IC₅₀	0.13 3 Compound: 21; AZD4205	Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA Inhibition of JAK1 in human NCI-H1975 cells assessed as decrease in STAT3 phosphorylation measured after 1 hr by ELISA	[PMID: 32297743]

In Vitro

Golidocitinib (Example 32) is a selective JAK1 inhibitor, with an IC₅₀ of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC₅₀, >14.7, >30 μM, respectively). Golidocitinib significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC₅₀ of 161 nM^[1].

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

In Vivo

Golidocitinib (12.5 mg/kg BID (twice daily), 25 m/kg BID or 50 mg/kg BID, p.o.) alone has increasing antitumor effects, and ehances the antitumor activity of osimertinib, compared to treatment with osimertinib alone in mice bearing NCI-H1975 cells^[1].

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

Ensayo clínico

Peso molecular

489.57

Fòrmula

C₂₅H₃₁N₉O₂

No. CAS

2091134-68-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

C[C@@H](N1CCN(C)CC1)C(NC2=C3C(C(C4=NC(NC5=CN(C)N=C5OC)=NC=C4)=CN3)=CC=C2)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (204.26 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	2.0426 mL	10.2130 mL	20.4261 mL
5 mM	0.4085 mL	2.0426 mL	4.0852 mL
10 mM	0.2043 mL	1.0213 mL	2.0426 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.

Calculadora de molaridad
Calculadora de dilución

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.5 mg/mL (5.11 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 (5.11 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 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: ≥ 2.5 mg/mL (5.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.

Pureza y Documentación

Purity: 99.54%

Select Batch:

Ficha de datos (273 KB) SDS (252 KB)

COA (249 KB) HNMR (513 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Annika Birgitta Margareta ÅSTRAND, et al. Compounds and methods for inhibiting jak. WO2017050938A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0426 mL	10.2130 mL	20.4261 mL	51.0652 mL
	5 mM	0.4085 mL	2.0426 mL	4.0852 mL	10.2130 mL
	10 mM	0.2043 mL	1.0213 mL	2.0426 mL	5.1065 mL
	15 mM	0.1362 mL	0.6809 mL	1.3617 mL	3.4043 mL
	20 mM	0.1021 mL	0.5107 mL	1.0213 mL	2.5533 mL
	25 mM	0.0817 mL	0.4085 mL	0.8170 mL	2.0426 mL
	30 mM	0.0681 mL	0.3404 mL	0.6809 mL	1.7022 mL
	40 mM	0.0511 mL	0.2553 mL	0.5107 mL	1.2766 mL
	50 mM	0.0409 mL	0.2043 mL	0.4085 mL	1.0213 mL
	60 mM	0.0340 mL	0.1702 mL	0.3404 mL	0.8511 mL
	80 mM	0.0255 mL	0.1277 mL	0.2553 mL	0.6383 mL
	100 mM	0.0204 mL	0.1021 mL	0.2043 mL	0.5107 mL

Golidocitinib Related Classifications

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:

Golidocitinib2091134-68-6AZD4205AZD 4205AZD-4205JAKJanus kinaseInhibitorinhibitorinhibit

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Golidocitinib (Synonyms: AZD4205)

Revisión del cliente

Other Forms of Golidocitinib:

Golidocitinib Related Antibodies

2 Publications Citing Use of MCE Golidocitinib

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas JAK:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Golidocitinib Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Golidocitinib Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

Request for HNMR Report

SAFETY DATA SHEET (SDS)

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