LJI308 |
| Catalog No.GC16601 |
LJI308 es un potente inhibidor de la cinasa S6 panribosÓmica (RSK), con IC50 de 6 nM, 4 nM y 13 nM para RSK1, RSK2 y RSK3, respectivamente. LJI308 inhibe la fosforilaciÓn de RSK (T359/S363) e YB-1 (S102) después de la irradiaciÓn, el tratamiento con EGF y en células que expresan una mutaciÓn KRAS.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1627709-94-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.004 to 0.013 mM for RSK1, 2, and 3.
LJI308 is a potent and selective inhibitor of RSK. The p90 ribosomal S6 kinase (RSK) comprises a family of serine/threonine kinase which is expressed in various human cancers. RSK is the cytosolic substrate for the ERK (extracellular sianal-regulated kinase), involved in direct regulation of cell survival, proliferation, and cell polarity. Previous studies have demonstrated that RSK pathway is important for the growth and proliferation of cancer stem cells [1,2].
The IC50 values of LJI308 against RSK1, 2, and 3 were about 0.004 - 0.013 mmol/L. 10 μM LJI308 could bind to nearly 100% of the RSK2. LJI308 bound the N-termini of RSK1, RSK3, and RSK4 to a similar extent. LJI308 inhibited S6K1 with an IC50 of 0.8 mM. In both MDA-MB-231 and H358 cell lines, 1 μM and 10 μM LJI308 exihibited an inhibitory effect on colony formation and cell growth with a different sensitivity [1]. In HTRY-LT cell lines, treating with LJI308 (1-10 µM) after 4 or 8 days decreased the cell viability by up to 90%; while little to no effect was observed in the non-tumorigenic HTRZ cells [2].
LJI308, the RSK inhibitor, could be used in combination with conventional chemotherapy to overcome the drug resistance and improve survival in patients with the triple-negative breast cancer (TNBC) [2].
References:
[1].Aronchik I, Appleton B A, Basham S E, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers[J]. Molecular Cancer Research, 2014, 12(5): 803-812.
[2].Davies A H, Reipas K, Hu K, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells[J]. Oncotarget, 2015, 6(24): 20570.
| Cas No. | 1627709-94-7 | SDF | |
| Chemical Name | 2,6-difluoro-4-(4-(4-morpholinophenyl)pyridin-3-yl)phenol | ||
| Canonical SMILES | FC1=C(O)C(F)=CC(C(C=NC=C2)=C2C3=CC=C(N4CCOCC4)C=C3)=C1 | ||
| Formula | C21H18F2N2O2 | M.Wt | 368.38 |
| Solubility | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7146 mL | 13.5729 mL | 27.1459 mL |
| 5 mM | 0.5429 mL | 2.7146 mL | 5.4292 mL |
| 10 mM | 0.2715 mL | 1.3573 mL | 2.7146 mL |
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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