Topotecan HCl
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 HCl(SKF104864)是拓扑异构酶1的抑制剂,是喜树碱(camptothecin)的半合成类似物[1]。
研究表明,在小鼠肿瘤模型中,Topotecan HCl(SKF104864)具有强效抗肿瘤活性。另外,Topotecan HCl对静脉植入P388白血病和静脉及皮下植入Lewis肺癌具有有效的效应。Topotecan HCl对皮下植入的实体瘤具有一定活性,包括化疗难治性肿瘤和人类异种移植HT-29结肠癌。相比喜树碱(camptothecin)和9-氨基喜树碱(9-amino-camptothecin),Topotecan HCl可以诱导肺癌模型(Lewis肺癌和B16黑色素瘤)的肿瘤消退。在临床前毒理学研究中,Topotecan HCl对迅速增殖的组织具有浓度依赖性的、可逆的和有限的毒性,例如骨髓和胃肠上皮[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 457.91 |
Cas No. | 119413-54-6 |
Formula | C23H24ClN3O5 |
Solubility | ≥22.9 mg/mL in DMSO; insoluble in EtOH; ≥2.14 mg/mL in H2O with gentle warming and ultrasonic |
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 hydrochloride |
SDF | Download SDF |
Canonical SMILES | Cl[H].O=C1N(C([H])([H])C2=C([H])C(C(C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=C3O[H])=C(C([H])=C3[H])N=C42)C4=C([H])C([C@@](C([H])([H])C([H])([H])[H])5O[H])=C1C([H])([H])OC5=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。 |
细胞实验: | |
细胞系 |
MCF-7乳腺癌细胞系、人前列腺癌细胞系(PC-3和LNCaP) |
溶解方法 |
该化合物在DMSO中的溶解度 > 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应时间 |
500 nM、持续6-12天; 或2、10 nM,持续72小时 |
应用 |
Topotecan处理的细胞在体外显示受损的球形成能力。Topotecan处理MCF-7细胞诱导的ABCG2表达与CD24/EpCAM表达降低相关[1]。此外,Topotecan以浓度依赖性方式增加PC-3和LNCaP细胞毒性 [2]。 |
动物实验: | |
动物模型 |
新生的NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG)小鼠或成年NMRI-nu/nu小鼠模型; PC-3异种移植模型 |
剂量 |
2.45和0.10 mg/kg/天、肿瘤内注射、连续输注或常规尾静脉注射给药,30天 |
应用 |
Topotecan处理的细胞降低免疫缺陷小鼠的致瘤性 [1]。 此外,低剂量连续给予Topotecan可增强前列腺癌的抗肿瘤活性 [2]。 |
注意事项 |
请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
References: 1. Huber, S., Wege, A. K., Bernhardt, G., Buschauer, A. and Brockhoff, G. (2015) Topotecan-induced ABCG2 expression in MCF-7 cells is associated with decreased CD24 and EpCAM expression and a loss of tumorigenicity. Cytometry A. 87, 707-716 2. Aljuffali, I. A., Mock, J. N., Costyn, L. J., Nguyen, H., Nagy, T., Cummings, B. S. and Arnold, R. D. (2011) Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Cancer Biol Ther. 12, 407-420 |
质量控制和MSDS
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