Erastin
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| カタログ番号GC16630 |
Erastinは細胞透過性のフェロプトーシス活性化剤であり、がん遺伝子RASを発現する細胞に選択的に作用する抗腫瘍剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 571203-78-6
Sample solution is provided at 25 µL, 10mM.
- Free Radical Bio Med (2024).PMID:39566750
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Erastinは細胞透過性のフェロプトーシス活性化剤であり、がん遺伝子RASを発現する細胞に選択的に作用する抗腫瘍剤である。
Erastinは、VDAC2/3に直接結合してミトコンドリア外膜の透過性を変化させ、NADHの酸化速度を低下させることにより、フェロプターシスを誘導する。Erastinは、標的効果を発揮するほか、特定のがん細胞における化学療法、標的療法、免疫療法を増強することから、がん細胞治療におけるErastinの役割の可能性が示唆されている。
Erastinとその類似体は、xc-系を介してシスチンの取り込みを特異的に阻害し、様々な細胞状況においてフェロプターシスを誘発し、SASよりもはるかに強力に作用した。さらに、HT-1080とCalu-1の両細胞において、ErastinはSASよりも約2500倍強力にxc-系の機能を阻害した（HT-1080：ErastinIC50＝0.20 µM、SAS IC50＝450 µM、Calu-1：ErastinIC50＝0.14 µM、SAS IC50＝460 µM）。
SLC7A11の阻害剤であるErastinは、in vitroおよびin vivoの実験により、大腸CSCsに対して著しく強い細胞毒性作用を示すことが判明した。さらに、Erastinは大腸がんCSCs（大腸がん幹細胞）の化学療法抵抗性を減弱させた。in vivo実験では、大腸がんマウスにErastin（10 mg/kg）を2日ごとに静脈注射した。その結果、ErastinはALDH1活性を阻害し、大腸がん細胞のスフィアのサイズと数を減少させることが判明した。
References:
[1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523.
[2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450.
[3]. Yang Y, et al. Nedd4 ubiquitylates VDAC2/3 to suppress erastin-induced ferroptosis in melanoma. Nat Commun. 2020 Jan 23;11(1):433.
| 細胞実験[1]: | |
細胞株 | 143B BJeHLT BJeLR Calu-1 HT-1080 |
準備方法 | DMSOに20 mMで溶解。 |
反応条件 | 10 μM、72時間 |
アプリケーション | エラスチンはシステインの取り込みを系統xc−を通じて抑制し、さまざまな細胞環境でフェロトーシスを誘発した。（HT-1080: エラスチンIC50 = 0.20 µM; Calu-1: エラスチンIC50 = 0.14 µM） |
| 動物実験 [2]: | |
動物モデル | BALB/cヌードマウス（大腸癌） |
準備方法 | DMSOに20 mMで溶解。 |
投与形態 | 10 mg/kg、静脈注射 |
アプリケーション | エラスチンはALDH1活性を抑制し、大腸癌細胞におけるスフェアサイズと数を減少させた。 |
参考文献: [1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523. [2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450. | |
| Cas No. | 571203-78-6 | SDF | |
| Chemical Name | 2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one | ||
| Canonical SMILES | O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5 | ||
| Formula | C30H31ClN4O4 | M.Wt | 547.04 |
| 溶解度 | ≥ 10.92mg/mL in DMSO with gentle warming ,This product is unstable in solution and it is recommended to prepare and use it immediately. | Storage | Store at -20° C |
| General tips | This product is unstable in nature and needs to be prepared and used immediately! It is recommended that you purchase small-sized packages, or repack small-sized ones after receiving the goods. | ||
| 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 | 1.828 mL | 9.1401 mL | 18.2802 mL |
| 5 mM | 0.3656 mL | 1.828 mL | 3.656 mL |
| 10 mM | 0.1828 mL | 0.914 mL | 1.828 mL |
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- Purity: >99.00%
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