Camptothecin (Synonyms: MAGCPT, NSC 94600) |
カタログ番号GC15439
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Camptothecinは特異的なDNAトポイソメラーゼI（Top1）阻害剤であり、IC50値は679nMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 7689-03-4
Sample solution is provided at 25 µL, 10mM.
Camptothecinは特異的なDNAトポイソメラーゼI（Top1）阻害剤であり、IC50値は679nMである[1]。CamptothecinはDNAの切断とタンパク質DNA架橋を誘発する植物アルカロイドである[2]。Camptothecinは、大腸、乳、肺と卵巣癌に対して有力な抗腫瘍活性を持つ[3]。
試験管内では、camptothecin (0.1-5µM)で高いTOP1酵素活性の乳癌由来の細胞（ルミナルサブタイプMCF7およびHER2サブタイプHCC1419）を72時間処理した結果、細胞の生存率を著しく阻害し、IC50値はそれぞれ0.089μMと0.067μMであった[4]。camptothecin (0.5µM)でHeLaとHEK293細胞を8-24時間処理した結果、低酸素誘発因子-1α(HIF-1α)の蓄積を著しく減らしたが、HIF-1βレベルを影響しなかった[5]。
生体内では、肥満のマウスにcamptothecin (1 mg/kg)で30日間処理した結果、マウスの肝臓における成長分化因子15（GDF15）の発見と分泌を誘発し、よって食物の取り込みを減らし、体重を正常化し、代謝障害を改善させた[6]。Camptothecin (2 mg/kg)で、黒色腫細胞の転移のマウスに処理した結果、肺の転移数を著しく減らした[7]。
References:
[1]Luzzio M J, Besterman J M, Emerson D L, et al. Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I[J]. Journal of medicinal chemistry, 1995, 38(3): 395-401.
[2]Stingele J, Jentsch S. DNA–protein crosslink repair[J]. Nature reviews Molecular cell biology, 2015, 16(8): 455-460.
[3]Huang Q, Wang L, Lu W. Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents[J]. European journal of medicinal chemistry, 2013, 63: 746-757.
[4]Tesauro C, Simonsen A K, Andersen M B, et al. Topoisomerase I activity and sensitivity to camptothecin in breast cancer-derived cells: a comparative study[J]. BMC cancer, 2019, 19: 1-15.
[5]Bertozzi D, Marinello J, Manzo S G, et al. The natural inhibitor of DNA topoisomerase I, camptothecin, modulates HIF-1α activity by changing miR expression patterns in human cancer cells[J]. Molecular cancer therapeutics, 2014, 13(1): 239-248.
[6]Lu J F, Zhu M Q, Xie B C, et al. Camptothecin effectively treats obesity in mice through GDF15 induction[J]. PLoS Biology, 2022, 20(2): e3001517.
[7]Schön M, Wienrich B G, Kneitz S, et al. KINK-1, a novel small-molecule inhibitor of IKKβ, and the susceptibility of melanoma cells to antitumoral treatment[J]. Journal of the National Cancer Institute, 2008, 100(12): 862-875.
| 細胞実験[1]: | |
細胞株 | MCF7 (ルミナルサブタイプ)、HCC1419 (HER2サブタイプ)細胞 |
準備方法 | 100μLの成長培地とともに96ウェルの平底のプレートで細胞を播種した。24時間後、細胞培地を培地のみ、DMSO培地またはCamptothecin（濃度範囲は0.1μMから5μM）に置き換え、72時間培養した。 |
反応条件 | 0.1-5µM；72時間 |
アプリケーション | TOP1酵素活性の高いMCF7（ルミナルサブタイプ）とHCC1419（HER2サブタイプ）はcamptothecinの処理に対して高い感受性を示し、IC50値はそれぞれ0.089 μMと0.067 μMである。 |
| 動物実験 [2]: | |
動物モデル | 雄Gfral+/+とGfral−/−マウス |
準備方法 | 8週齢のマウスをHFDで5週間維持させた。各マウスにCamptothecin (1mg/kg)を30日間経口投与し、体重と食物の摂取量は3日に一回監視した。 |
投与形態 | 1mg/kg; p.o. |
アプリケーション | Camptothecinはマウスの肝臓におけるGDF15細胞の発見と分泌を誘発し、よって食物の取り込みを減らし、肥満のマウスの体重を正常化し、代謝障害を逆転させた。 |
References: | |
| Cas No. | 7689-03-4 | SDF | |
| 同義語 | MAGCPT, NSC 94600 | ||
| Chemical Name | (S)-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione | ||
| Canonical SMILES | O=C(N(CC1=CC(C=CC=C2)=C2N=C13)C3=C4)C(CO5)=C4[C@@](O)(CC)C5=O | ||
| Formula | C20H16N2O4 | M.Wt | 348.35 |
| 溶解度 | 10mg/mL in 1M NaOH;6.7mg/mL in DMSO | Storage | 4°C, protect from light |
| 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 | 2.8707 mL | 14.3534 mL | 28.7068 mL |
| 5 mM | 574.1 μL | 2.8707 mL | 5.7414 mL |
| 10 mM | 287.1 μL | 1.4353 mL | 2.8707 mL |
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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.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)