Topotecan
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Topotecan(SKF104864)是拓扑异构酶1的抑制剂,是喜树碱的半合成类似物[1].
Topotecan(SKF104864)在小鼠模型中具有有效的抗肿瘤活性.此外,Topotecan对静脉注射植入的P388白血病和静脉注射及皮下植入的Lewis肺癌也有效.Topotecan对皮下植入的实体瘤,包括耐药肿瘤和人类结肠癌异种移植物HT-29也有抗癌活性.相比喜树碱和9-氨基喜树碱,Topotecan可在肺肿瘤模型(Lewis肺癌和B16黑色素瘤)中诱导肿瘤消退.在临床前毒理学研究中,Topotecan对快速增值的组织如骨髓和胃肠上皮具有浓度依赖的可逆的有限毒性[1].
参考文献：
[1] Creemers GJ1, Lund B, Verweij J. Topoisomerase I inhibitors: topotecan and irenotecan. Cancer Treat Rev. 1994 Jan;20(1):73-96.
- 1. Lambo S, Gröbner SN, et al. "The molecular landscape of ETMR at diagnosis and relapse." Nature. 2019 Dec;576(7786):274-280. PMID:31802000
- 2. Manasi Ratnaparkhe, John Wong, et al. "Defective DNA damage repair leads to frequent catastrophic genomic events in murine and human tumors." bioRxiv. 2018 May 4.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 421.45 |
| Cas No. | 123948-87-8 |
| Formula | C23H23N3O5 |
| Solubility | ≥21.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | (S)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione |
| SDF | Download SDF |
| Canonical SMILES | CC[C@]1(O)C(C=C2C3=NC4=CC=C(O)C(CN(C)C)=C4C=C3CN2C5=O)=C5COC1=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
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Cell lines |
Human glioma cell lines U251, U87, GSCs-U251 and GSCs-U87 |
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Reaction Conditions |
0.02, 0.2, 2, 20 or 40 μmol/L topotecan for 12, 24 or 48 h incubation |
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Applications |
Topotecan obviously inhibited proliferation of not only human glioma cells but also glioma stem cells in a dose- and time-dependent manner. In addition, topotecan (3 μmol/L, 24 h) induced cell cycle arrest in G0/G1 and S phases and promoted apoptosis. |
| Animal experiment:[2] | |
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Animal models |
Mouse models of aggressive pediatric solid tumor |
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Dosage form |
1 mg/kg Once daily by oral gavage |
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Applications |
Metronomic administration of topotecan and pazopanib showed a statistically significant antitumor activity compared with respective single agents in pediatric tumor mouse models, representing a valid option as a maintenance therapy in aggressive pediatric solid tumors. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Zhang FL, Wang P, Liu YH, et al. Topoisomerase I inhibitors, shikonin and topotecan, inhibit growth and induce apoptosis of glioma cells and glioma stem cells. PLoS One, 2013, 8(11): e81815. 2. Kumar S, Mokhtari RB, Sheikh R, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clinical Cancer Research, 2011, 17(17): 5656-5667. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
