GSK 2837808A |
カタログ番号GC13464 |
GSK 2837808Aは選択的な乳酸脱水素酵素A(LDHA)の阻害剤であり、hLDHAとhLDHBに対するIC50はそれぞれ2.6nM、43nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1445879-21-9
Sample solution is provided at 25 µL, 10mM.
GSK 2837808Aは選択的な乳酸脱水素酵素A(LDHA)の阻害剤であり、hLDHAとhLDHBに対するIC50はそれぞれ2.6nM、43nMである[1]。
GSK2837808A(10 µM;24-72h)は有酸素糖分解、増殖、細胞周期およびアポトーシス抵抗を促進することによって、セントロメアタンパク質N(CENP-N)過剰発現によるNPC細胞への影響を遮断する[2]。GSK2837808A(0, 5, 10, 20 µM)はLDHAを阻害することで低ATP/AMP比を逆転し、高レベルのアデノシン一リン酸活性化プロテインキナーゼ (AMPK) を活性化し、HAS2の合成およびヒアルロン酸(HA)産生状況TMJ変形性関節炎滑膜線維芽細胞(TMJOA SF)を混乱させる[3]。
GSK2837808A(6 mg/kg/day;p.o;4週間)治療の後、KPCとCAF鼠の腫瘍重量およびサイズが顕著に低下し、腫瘍乳酸と乳酸:ピルビン酸の比が有意に低下し、腫瘍細胞のアポトーシスが増加する[4]。
References:
[1]. Billiard J, Dennison JB, et,al. Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells. Cancer Metab. 2013 Sep 6;1(1):19. doi: 10.1186/2049-3002-1-19. PMID: 24280423; PMCID: PMC4178217.
[2]. Qi CL, Huang ML, et,al. The IRF2/CENP-N/AKT signaling axis promotes proliferation, cell cycling and apoptosis resistance in nasopharyngeal carcinoma cells by increasing aerobic glycolysis. J Exp Clin Cancer Res. 2021 Dec 10;40(1):390. doi: 10.1186/s13046-021-02191-3. PMID: 34893086; PMCID: PMC8662847.
[3]. Li HM, Guo HL, et,al. Inhibition of glycolysis by targeting lactate dehydrogenase A facilitates hyaluronan synthase 2 synthesis in synovial fibroblasts of temporomandibular joint osteoarthritis. Bone. 2020 Dec;141:115584. doi: 10.1016/j.bone.2020.115584. Epub 2020 Aug 11. PMID: 32795674.
[4].Gupta VK, Sharma NS, et,al. Hypoxia-Driven Oncometabolite L-2HG Maintains Stemness-Differentiation Balance and Facilitates Immune Evasion in Pancreatic Cancer. Cancer Res. 2021 Aug 1;81(15):4001-4013. doi: 10.1158/0008-5472.CAN-20-2562. Epub 2021 May 14. PMID: 33990397; PMCID: PMC8338764.
細胞実験[1]: | |
細胞株 | NPC (鼻咽頭) 細胞 |
準備方法 | |
反応条件 | 10 µM;24-72h |
アプリケーション | GSK2837808A(10 µM;24-72h)は有酸素糖分解、増殖、細胞周期およびアポトーシス抵抗を促進することによって、セントロメアタンパク質N(CENP-N)過剰発現によるNPC細胞への影響を遮断する。 |
動物実験 [2]: | |
動物モデル | メス C57BL/6 鼠 |
準備方法 | 腫瘍(KPCおよびCAF細胞)を10日間成長させる。一つ鼠の群にGSK2837808Aを毎日6mg/kgの投与量で経口投与し、一方で別の群は载体对照を受ける。 |
投与形態 | 6 mg/kg/day; p.o ;4週間 |
アプリケーション | GSK2837808Aは腫瘍重量およびサイズが顕著に低下し、腫瘍細胞のアポトーシスが増加する。 |
References: |
Cas No. | 1445879-21-9 | SDF | |
Chemical Name | 3-((3-(N-cyclopropylsulfamoyl)-7-(2,4-dimethoxypyrimidin-5-yl)quinolin-4-yl)amino)-5-(3,5-difluorophenoxy)benzoic acid | ||
Canonical SMILES | O=S(C(C=N1)=C(NC2=CC(OC3=CC(F)=CC(F)=C3)=CC(C(O)=O)=C2)C(C1=C4)=CC=C4C5=CN=C(OC)N=C5OC)(NC6CC6)=O | ||
Formula | C31H25F2N5O7S | M.Wt | 649.62 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,Ethanol: slightly soluble | 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 | 1.5394 mL | 7.6968 mL | 15.3936 mL |
5 mM | 0.3079 mL | 1.5394 mL | 3.0787 mL |
10 mM | 0.1539 mL | 0.7697 mL | 1.5394 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
(Based on Reviews and 1 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *