IN 1130 |
| Catalog No.GC50317 |
IN 1130 est un inhibiteur hautement sélectif de la kinase du récepteur du facteur de croissance transformant β de type I (ALK5) avec une IC50 de 5,3 nM pour la phosphorylation de Smad3 médiée par ALK5.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 868612-83-3
Sample solution is provided at 25 µL, 10mM.
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Potent and selective inhibitor of TGF-β type I receptor (ALK5). Inhibits Smad-2 phosphorylation (IC50 = 5.3 nM). Exhibits selectivity over a panel of 27 serine/ threonine and tyrosine kinases including P38α. Attenuates TGFβ/Smad signaling, cell migration, invasion, lung metastasis and increases survival of mice in 4TI in vivo models. Suppresses renal fibrosis in obstructive nephropathy in vivo models.
Moon et al (2006) IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 70 1234 PMID:16929250 |Lee et al (2008) Effect of IN-1130, a small molecule inhibitor of transforming growth factor-beta type I receptor/AVNreceptor-like kinase-5, on prostate cancer cells. J.Urol. 180 2660 PMID:18951571 |Park et al (2014) An novel inhibitor of TGF-beta type I receptor, IN-1130, blocks breast cancer lung metastasis through inhibition of epithelial-mesenchymal transition. Cancer Lett. 351 72 PMID:24887560
| Cas No. | 868612-83-3 | SDF | |
| Canonical SMILES | CC1=NC(C2=C(C3=CC4=C(N=CC=N4)C=C3)NC(CC5=CC(C(N)=O)=CC=C5)=N2)=CC=C1 | ||
| Formula | C25H20N6O | M.Wt | 420.47 |
| Solubility | DMSO : 100 mg/mL (237.83 mM; Need ultrasonic) | Storage | Store 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. |
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| 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 | 2.3783 mL | 11.8915 mL | 23.7829 mL |
| 5 mM | 475.7 μL | 2.3783 mL | 4.7566 mL |
| 10 mM | 237.8 μL | 1.1891 mL | 2.3783 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 ddH2O, 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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