货号:A122669
同义名:
盐酸拓扑替康
/ SKF 104864A hydrochloride;NSC 609669 hydrochloride
Topotecan HCl(SKF 104864A Hydrochloride)作为一种拓扑异构酶I抑制剂,具有强效抗肿瘤活性。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ellagic acid | ✔ | 99%+ | |||||||||||||||||
β-Lapachone | ✔ | 99%+ | |||||||||||||||||
(s)-10-hydroxycamptothecin | ✔ | 99%+ | |||||||||||||||||
Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
99%+ | |||||||||||||||||
Topotecan |
++++
Topo I (DU-145 Luc cells), IC50: 2 nM Topo I (MCF-7 Luc cells), IC50: 13 nM |
99%+ | |||||||||||||||||
Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
SN-38 | ✔ | 98% | |||||||||||||||||
Levofloxacin hydrate | ✔ | 99%+ | |||||||||||||||||
Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
Ofloxacin | ✔ | 98+% | |||||||||||||||||
Enoxacin | ✔ | 99%+ | |||||||||||||||||
Flumequine |
+
Topo II, IC50: 15 μM |
99%+ | |||||||||||||||||
Levofloxacin | ✔ | 99%+ | |||||||||||||||||
Etoposide | ✔ | 98% | |||||||||||||||||
Pefloxacin mesylate dihydrate | ✔ | 99+% | |||||||||||||||||
Marbofloxacin | ✔ | 99%+ | |||||||||||||||||
Voreloxin HCl | ✔ | 98% | |||||||||||||||||
Mitoxantrone dihydrochloride | ✔ | PKC | 99%+ | ||||||||||||||||
Nalidixic acid | ✔ | 99%+ | |||||||||||||||||
Doxorubicin | ✔ | 98% | |||||||||||||||||
Novobiocin sodium | ✔ | 98%+ | |||||||||||||||||
Amonafide | ✔ | 99%+ | |||||||||||||||||
Pirarubicin | ✔ | 98%+ | |||||||||||||||||
Idarubicin HCl |
+++
Topo II (MCF-7 cells), IC50: 3.3 ng/mL |
99%+ | |||||||||||||||||
Genistein | ✔ | EGFR | 98% | ||||||||||||||||
Teniposide | ✔ | 98% | |||||||||||||||||
Moxifloxacin | ✔ | 98% | |||||||||||||||||
Ciprofloxacin | ✔ | 99%+ | |||||||||||||||||
Clinafloxacin | ✔ | 97% | |||||||||||||||||
Gatifloxacin | ✔ | 99%+ | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Epirubicin HCl | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Topotecan Hydrochloride (SKF 104864A Hydrochloride) effectively inhibits the proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner. An optimal administration concentration of 3 μM is selected based on IC50 values at 24 h. Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Additionally, it inhibits cell viability in a dose-dependent manner [1]. |
体内研究 | In the NUB-7 metastatic model, animals from all four groups are sacrificed after 14 days of treatment. Compared to the control group, low dose metronomic (LDM) Topotecan Hydrochloride and TP+Pazopanib (PZ) result in significantly lower liver weights in TP+PZ-treated animals compared to PZ alone. Microscopic tumors are observed in the livers of mice in all groups except TP+PZ, indicating the ability of Topotecan Hydrochloride+PZ to control liver metastasis. In previous dose-response studies, daily oral metronomic Topotecan Hydrochloride (0.5, 1.0, and 1.5 mg/kg) showed greater reduction in microvascular density compared to weekly maximum-tolerated dose regimen (7.5 and 15 mg/kg) in an ovarian cancer model. However, mice treated with 1.5 mg/kg daily oral Topotecan Hydrochloride exhibited decreased food intake and a lesser antitumor effect [2]. |
体外研究 | Topotecan Hydrochloride (SKF 104864A Hydrochloride) effectively inhibits the proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner. An optimal administration concentration of 3 μM is selected based on IC50 values at 24 h. Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Additionally, it inhibits cell viability in a dose-dependent manner [1]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
A427 human lung carcinoma | Proliferation assay | Antiproliferative activity measured against A427 human lung carcinoma, IC50=49 nM | 9876111 | ||
COR-L23/P cell | Cytotoxic assay | Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line, IC50=13.2 nM | 11806724 | ||
HeLa cells | Growth inhibition assay | Growth inhibition of HeLa cells after 4 days, GI50=30 nM | 17418582 | ||
HT-29 cells | Cytotoxic assay | Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay, IC50=25 nM | 7853331 | ||
Dose | Rat: 0.23 mg/kg[3] (i.v.), 0.7 mg/kg[4] (i.v.); 0.14 mg/kg, 0.79 mg/kg[4] (inh.); 10 ml/kg[5] (p.o.) Dog: 0.068 mg/kg - 0.2 mg/kg[5] (p.o.) Mice: 0.5 mg/kg - 1.5 mg/kg[6] (p.o.) | ||||||||||||||
Administration | i.v., inh., p.o. | ||||||||||||||
Pharmacokinetics |
|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00231855 | Ovarian Neoplasms ... 展开 >> Uterine Neoplasms 收起 << | Phase 2 | Completed | - | United States, New York ... 展开 >> Montefiore Medical Center Bronx, New York, United States, 10461 收起 << |
NCT00466232 | Small Cell Carcinoma ... 展开 >> Lung Cancer 收起 << | Phase 1 | Completed | - | United States, Minnesota ... 展开 >> Park Nicollet Institute St. Louis Park, Minnesota, United States, 55416 收起 << |
NCT00170625 | Ovarian Cancer | Phase 1 Phase 2 | Completed | - | - |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.18mL 0.44mL 0.22mL |
10.92mL 2.18mL 1.09mL |
21.84mL 4.37mL 2.18mL |
CAS号 | 119413-54-6 |
分子式 | C23H24ClN3O5 |
分子量 | 457.907 |
别名 | 盐酸拓扑替康 ;SKF 104864A hydrochloride;NSC 609669 hydrochloride;SKF 104864A;NSC 609669;Topotecan (hydrochloride);NSC 609699;SKFS 104864A;Nogitecan HCl;Topotecan HCl |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(229.3 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 30 mg/mL(65.52 mM),配合低频超声助溶 |
动物实验配方 |
PO 0.5% CMC-Na 33 mg/mL suspension |