TCS 21311 (Synonyms: NIBR3049) |
Catalog No.GC16584
One-Click Copy Product Info
|
A JAK3 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1260181-14-3
Sample solution is provided at 25 µL, 10mM.
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TCS 21311 is a potent and selective JAK3 inhibitor with the IC50 values of 8 nM. TCS 21311 shows high selectivity for JAK3 over JAK1, JAK2 and TYK2. The IC50 values are 1017, 2550 and 8055 nM respectively. TCS 21311 exihibits inhibitory effect on GSK-3β, PKCα and PKCθ with the IC50 values of 3, 13 and 68 nM, respectively [1].
Janus kinases (JAK) belong to a small family of cytoplasmic protein tyrosine kinases including JAK1, JAK2, Tyk2, and JAK3, which play important roles in initiating the cytokine-triggered signaling events by activators of transcription (STAT) proteins via tyrosine phosphorylation [2]. Due to its association with relevant cytokine signaling pathways, JAK3 serves as an important target for therapeutic intervention in the treatment of inflammatory diseases, autoimmune disorders and organ transplant rejection [2].
References:
[1] Thoma G, Nuninger F, Falchetto R, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family[J]. Journal of medicinal chemistry, 2010, 54(1): 284-288.
[2] Clark M P, George K M, Bookland R G, et al. Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3)[J]. Bioorganic & medicinal chemistry letters, 2007, 17(5): 1250-1253.
| Cas No. | 1260181-14-3 | SDF | |
| Synonyms | NIBR3049 | ||
| Chemical Name | 3-[5-[4-(2-hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione | ||
| Canonical SMILES | CC(C)(C(=O)N1CCN(CC1)C2=CC(=C(C=C2)C(F)(F)F)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54)O | ||
| Formula | C27H25F3N4O4 | M.Wt | 526.51 |
| Solubility | <52.65mg/ml in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8993 mL | 9.4965 mL | 18.993 mL |
| 5 mM | 379.9 μL | 1.8993 mL | 3.7986 mL |
| 10 mM | 189.9 μL | 949.6 μL | 1.8993 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)