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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。

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GSK 2837808A 化学構造

Cas No.: 1445879-21-9

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$210.00
在庫あり
2mg
$67.00
在庫あり
5mg
$126.00
在庫あり
10mg
$203.00
在庫あり
25mg
$406.00
在庫あり
50mg
$651.00
在庫あり
100mg
$1,036.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Description of GSK 2837808A

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.

Protocol of GSK 2837808A

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:
[1]. 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.
[2]. 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.

Chemical Properties of GSK 2837808A

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.

Complete Stock Solution Preparation Table of GSK 2837808A

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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
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In vivo Formulation Calculator (Clear solution) of GSK 2837808A

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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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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