Axitinib (AG 013736) (Synonyms: AG 013736) |
カタログ番号GC12216
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Axitinib (AG 013736)は経口活性の特異性血管内皮成長因子受容体（VEGFR）阻害剤であり、VEGFR-1、VEGFR-2とVEGFR-3を標的とし、IC50値はそれぞれ0.1nM、0.2nMと0.1-0.3nMである。
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Cas No.: 319460-85-0
Sample solution is provided at 25 µL, 10mM.
Axitinib (AG 013736)は経口活性の特異性血管内皮成長因子受容体（VEGFR）阻害剤であり、VEGFR-1、VEGFR-2とVEGFR-3を標的とし、IC50値はそれぞれ0.1nM、0.2nMと0.1-0.3nMである[1]。Axitinibは血小板由来の成長因子受容体(PDGFR)とチロシンタンパク質キナーゼKIT (c-KIT)に対し阻害作用を有し、IC50値はそれぞれ1.6nMと1.7nMである[2]。AxitinibはVEGFシグナル伝達経路を阻害することで、腫瘍の血管新生を阻害でき、よって腫瘍の成長と転移を阻害する[3]。Axitinibは癌の研究に常用され、特には腎細胞癌と甲状腺癌の治療に広く使われている[4]。
体外で、Axitinib (0.1-25μM)でヒト網膜内皮細胞(HRECs)を48時間処理した結果、細胞内乳糖脱水素酵素（LDH）の放出を著しく増やした。Axitinib (0.1, 1μM)は、持続的な高グルコース濃度と変動するグルコース濃度に暴露されるHRECsにおけるVEGFR2のリン酸化を著しく減らした[5]。
体内で、Axitinib (1mg/kg/日)で間質性膀胱炎（IC）ラットに5日間経口投与した結果、非尿路収縮を減らし、排尿間隔と尿量を増やし、尿路上皮剥離、血管新生、肥満細胞浸潤と線維症を緩和させた[6]。Axitinib (25mg/kg/日)をRenca細胞異種移植マウスに経口投与した結果、腫瘍の成長と転移を著しく阻害し、マウスでCD8+ T細胞の浸潤と活性を促進した[7]。
References:
[1] Malekan M, Ebrahimzadeh M A. Vascular endothelial growth factor receptors [VEGFR] as target in breast cancer treatment: current status in preclinical and clinical studies and future directions[J]. Current Topics in Medicinal Chemistry, 2022, 22(11): 891-920.
[2] Jiang D, Xu T, Zhong L, et al. Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases[J]. European Journal of Medicinal Chemistry, 2023, 257: 115535.
[3] Kelly R J, Rixe O. Axitinib—a selective inhibitor of the vascular endothelial growth factor (VEGF) receptor[J]. Targeted oncology, 2009, 4: 297-305.
[4] Keating G M. Axitinib: a review in advanced renal cell carcinoma[J]. Drugs, 2015, 75: 1903-1913.
[5] Lazzara F, Conti F, Sasmal P K, et al. Anti-angiogenic and antioxidant effects of axitinib in human retinal endothelial cells: implications in diabetic retinopathy[J]. Frontiers in Pharmacology, 2024, 15: 1415846.
[6] Shin J H, Ryu C M, Yu H Y, et al. Therapeutic effects of axitinib, an anti-angiogenic tyrosine kinase inhibitor, on interstitial cystitis[J]. Scientific Reports, 2023, 13(1): 8329.
[7] Yuan H, Cai P, Li Q, et al. Axitinib augments antitumor activity in renal cell carcinoma via STAT3-dependent reversal of myeloid-derived suppressor cell accumulation[J]. Biomedicine & Pharmacotherapy, 2014, 68(6): 751-756.
| 細胞実験[1]: | |
細胞株 | ヒト網膜内皮細胞(HRECs) |
準備方法 | 高レベルのグルコース(HG) (40mM)のある/ない状態で、Axitinib (0.1, 1, 10, 25µM)で、HRECsを新鮮な培地に48時間処理した。CyQUANTTM LDH細胞毒性アッセイを使い、乳糖脱水素酵素（LDH）細胞の放出を測定した。 |
反応条件 | 0.1, 1, 10, 25µM；48時間 |
アプリケーション | 濃度が25µMのAxitinibがHRECsに有毒で、対照細胞に比べて、著しいLDH放出に導くことが観察された。 |
| 動物実験 [2]: | |
動物モデル | Sprague Dawleyラット |
準備方法 | 10週齢の雌Sprague Dawleyラットを三つのグループ（n=10/グループ）に分けた：模擬手術、塩酸塩(HCl)とAxitinibグループである。HCl注射の一週間後（0日目）、AxitinibグループにAxitinib (1mg/kg)を5日間連続で経口投与し、痛みを毎日評価した。膀胱の機能、組織学、遺伝学の検査を7日目に評価した。 |
投与形態 | 1mg/kg/日；5日間；経口 |
アプリケーション | Axitinib投与の3日後に、疼痛閾値は著しく改善した。Axitinibは非排尿性収縮を減らし、排尿間隔と排尿量を増やし、尿路上皮剥離、血管新生、肥満細胞浸潤と線維症を軽減した。 |
References: | |
| Cas No. | 319460-85-0 | SDF | |
| 同義語 | AG 013736 | ||
| Chemical Name | N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide | ||
| Canonical SMILES | CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)C=CC4=CC=CC=N4 | ||
| Formula | C22H18N4OS | M.Wt | 386.47 |
| 溶解度 | ≥ 19.3mg/mL in DMSO | 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 | 2.5875 mL | 12.9376 mL | 25.8752 mL |
| 5 mM | 517.5 μL | 2.5875 mL | 5.175 mL |
| 10 mM | 258.8 μL | 1.2938 mL | 2.5875 mL |
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)