Golidocitinib
Based on 2 publication(s) in Google Scholar
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).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.54%
- CAS No.: 2091134-68-6
- Formule: C25H31N9O2
- Masse moléculaire:489.57
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
JAK/STAT Compound Library
HY-L008
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Stem Cell Signaling Compound Library
HY-L017
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Differentiation Inducing Compound Library
HY-L038
-
Reprogramming Compound Library
HY-L039
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Anti-Obesity Compound Library
HY-L087
-
Targeted Diversity Library
HY-L099
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Autoimmune Disease Compound Library
HY-L156
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Hematopathy Compound Library
HY-L171
-
Bioactive Compound Library Max
HY-L181
-
Epigenetics Compound Library Mini
HY-L005M
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Golidocitinib
More
Activité biologique
|
JAK1 73 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
0.13 μM
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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2091134-68-6
-
Appearance Solid
-
Masse moléculaire 489.57
-
Formule C25H31N9O2
-
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
-
Synonyms
AZD4205
-
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
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Cell
Cancer SLC6A6-mediated taurine uptake transactivates immune checkpoint genes and induces exhaustion in CD8+ T cells. [Abstract]2024 Apr 25;187(9):2288-2304.e27. PMID: 38565142 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Fiche technique (273 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instruction de manipulation (2659 KB)
Références
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.
| 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 |
Powered by Bioz