LXS196 (Synonyms: LXS196; IDE196) |
| カタログ番号GC32811 |
LXS196 (LXS196) は、1.9 nM、0.4 nM、および 3.1 μ の IC50 値を持つ、強力で選択的な経口活性プロテインキナーゼ C (PKC) 阻害剤です。および GSK3β、それぞれ。 LXS196 は、ブドウ膜黒色腫研究の可能性を秘めています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1874276-76-2
Sample solution is provided at 25 µL, 10mM.
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LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. It can be used for the treatment of uveal melanoma[1][2].
Upon oral administration, protein kinase C inhibitor LXS196 binds to and inhibits PKC, which prevents the activation of PKC-mediated signaling pathways. This may lead to the induction of cell cycle arrest and apoptosis in susceptible tumor cells. PKC, a serine/threonine protein kinase overexpressed in certain types of cancer cells, is involved in tumor cell differentiation, proliferation, invasion and survival[1].
LXS196 (compound 9) (15, 30, 75, 150 mg/kg, P.O., mice) shows improved efficacy (regression) in a 92.1 GNAQ uveal melanoma xenograft model in a dose-dependently manner[2].|| Animal Model:|Mice implanted with 92.1 GNAQ mutant uveal melanoma cells[2].|Dosage:|15, 30, 75, 150 mg/kg|Administration:|P.O. (bid) for 35 days|Result:|Dose-dependently suppressed the tumor growth.
[1]. Protein Kinase C Inhibitor LXS196 [2]. US20180179181.
| Cas No. | 1874276-76-2 | SDF | |
| 同義語 | LXS196; IDE196 | ||
| Canonical SMILES | NC1=C(C(NC2=C(N3CCC(C)(N)CC3)C=CC=N2)=O)N=C(C4=NC=CC=C4C(F)(F)F)C=N1 | ||
| Formula | C22H23F3N8O | M.Wt | 472.47 |
| 溶解度 | DMSO : ≥ 100 mg/mL (211.65 mM) | 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. |
||
| 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 | 2.1165 mL | 10.5827 mL | 21.1654 mL |
| 5 mM | 423.3 μL | 2.1165 mL | 4.2331 mL |
| 10 mM | 211.7 μL | 1.0583 mL | 2.1165 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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