Topotecan HCl
别名: Nogitecan HCl, SKFS 104864A, NSC 609699 中文名称：盐酸托泊替康
Topotecan HCl是一种拓扑异构酶I抑制剂，作用于MCF-7 Luc细胞和DU-145 Luc细胞，无细胞试验中IC50分别为13 nM和2 nM。Topotecan HCl 可诱导自噬和凋亡。
Topotecan HCl Chemical Structure
CAS: 119413-54-6
产品质控
批次：
纯度：
99.98%
99.98
Topotecan HCl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HeLa | Apoptosis assay | 0.8 to 1.6 uM | 24 hrs | Induction of apoptosis in human HeLa cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA | 24980118 |
| MDA-MB-231 | Apoptosis assay | 0.8 to 1.6 uM | 24 hrs | Induction of apoptosis in human MDA-MB-231 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA | 24980118 |
| A375 | Apoptosis assay | 0.8 to 1.6 uM | 24 hrs | Induction of apoptosis in human A375 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA | 24980118 |
| Caco2 | Apoptosis assay | 0.8 to 1.6 uM | 24 hrs | Induction of apoptosis in human Caco2 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA | 24980118 |
| human MDA-MB-435 cells | Cytotoxic assay | 72 h | Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay, GI50=34 nM | 22867019 | |
| human A2780 cells | Cytotoxic assay | 72 h | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50=33 nM | 24900725 | |
| human MOLT4 cells | Cytotoxic assay | 72 h | Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=19 nM | 24900725 | |
| human LoVo cells | Cytotoxic assay | 72 h | Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50=20 nM | 20371183 | |
| human NCI-H460 cells | Proliferation assay | 72 h | Antiproliferative activity against human NCI-H460 cells after 72 hrs by coulter counter analysis, IC50=16 nM | 21783369 | |
| human A375 cells | Cytotoxic assay | 72 h | Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50=13 nM | 21341674 | |
| human LNCAP cells | Cytotoxic assay | 72 h | Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50=9 nM | 21341674 | |
| human A2780 cells | Cytotoxic assay | 72 h | Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay, IC50=6 nM | 22959246 | |
| human H69 cells | Cytotoxic assay | 72 h | Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50=6 nM | 21341674 | |
| human A549 cells | Function assay | 4 h | Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50=5 nM | 18207748 | |
| human Ketr3 cells | Cytotoxic assay | 96 h | Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay, IC50=4.9 nM | 15165144 | |
| human MESSA cells | Cytotoxic assay | 72 h | Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay, IC50=4 nM | 21341674 | |
| human BGC823 cells | Cytotoxic assay | 96 h | Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay, IC50=4.3 nM | 15165144 | |
| human A549 cells | Cytotoxic assay | 96 h | Cytotoxicity against human A549 cells after 96 hrs by MTT assay, IC50=3.2 nM | 15165144 | |
| human MCF7 cells | Cytotoxic assay | 96 h | Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay, IC50=1.8 nM | 15165144 | |
| human HCT8 cells | Cytotoxic assay | 96 h | Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay, IC50=1.5 nM | 15165144 | |
| human Bel7402 cells | Cytotoxic assay | 96 h | Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay, IC50=1.2 nM | 15165144 | |
| human MDA-MB-435 cells | Cytotoxic assay | 72 h | Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, ic50=1 nM | 20371183 | |
| human U251 cells | Function assay | 6-24 h | Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis, EC50=54 nM | 22305612 | |
| human HepG2 cells | Cytotoxic assay | 4 days | Cytotoxicity against human HepG2 cells after 4 days by MTT assay, IC50=60 nM | 18554906 | |
| human KB cells | Cytotoxic assay | 72 h | Cytotoxicity against human KB cells after 72 hrs sulforhodamine B colorimetric assay, IC50=62.5 nM | 25008456 | |
| human HCT8 cells | Cytotoxic assay | 3 days | Cytotoxicity against human HCT8 cells after 3 days by MTT assay, IC50=70 nM | 20392545 | |
| human GBM2 cells | Proliferation assay | 72 h | Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.13 μM | 26355532 | |
| SK-MEL-2 cells | Cytotoxic assay | 72 h | Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay, IC50=0.14 μM | 21341674 | |
| human IGROV1 cells | Cytotoxic assay | 72 h | Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay, IC50=0.16 μM | 21341674 | |
| human U87 cells | Proliferation assay | 48 h | Antiproliferative activity against human U87 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.16 μM | 24826818 | |
| human HT1080 cells | Proliferation assay | 48 h | Antiproliferative activity against human HT1080 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay, IC50=0.18 μM | 26408815 | |
| human Hep3B cells | Proliferation assay | 72 h | Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50=0.22 μM | 19796956 | |
| human GBM3 cells | Proliferation assay | 72 h | Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.38 μM | 26355532 | |
| human KBVIN cells | Cytotoxic assay | 72 h | Cytotoxicity against human KBVIN cells after 72 hrs by SRB assay, IC50=0.4 μM | 25438769 | |
| human GBM1 cells | Proliferation assay | 72 h | Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.46 μM | 26355532 | |
| human U937 cells | Cytotoxic assay | 48 h | Cytotoxicity against human U937 cells expressing p53 mutant after 48 hrs by SRB assay ， IC50=1.1 μM | 19715319 | |
| Caco2 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay, IC50=0.119μM. | 24980118 | |
| Jurkat | Cytotoxicity assay | 24 hrs | Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay, IC50=0.127μM. | 24980118 | |
| A375 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human A375 cells after 24 hrs by MTT assay, IC50=0.162μM. | 24980118 | |
| HeLa | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HeLa cells after 24 hrs by MTT assay, IC50=0.38μM. | 24980118 | |
| MDA-MB-231 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.473μM. | 24980118 | |
| NCI-H460 | Antiproliferative assay | 1 hr | Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium, IC50=0.61μM. | 19530720 | |
| HCT8 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT8 cells after 48 hrs by CCK8 assay, IC50=1.875μM. | 25481395 | |
| KB | Antiproliferative assay | 48 hrs | Antiproliferative activity against human KB cells after 48 hrs by CCK8 assay, IC50=2.282μM. | 25481395 | |
| SGC7901 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human SGC7901 cells after 48 hrs by CCK8 assay, IC50=2.292μM. | 25481395 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay, IC50=4.208μM. | 25481395 | |
| A427 human lung carcinoma | Proliferation assay | Antiproliferative activity measured against A427 human lung carcinoma, IC50=49 nM | 9876111 | ||
| mouse P388 cells | Cytotoxic assay | Cytotoxicity against mouse P388 cells after MTT assay, IC50=45 nM | 18829334 | ||
| human KB3-1 cells | Cytotoxic assay | Cytotoxicity against human KB3-1 cells after MTT assay, IC50=40 nM | 18829334 | ||
| human stomach cancer cell line (MKN45) | Cytotoxic assay | In Vitro cytotoxicity against human stomach cancer cell line (MKN45), IC50=38 nM | 11334569 | ||
| human MES-SA/Dx5 cells | Cytotoxic assay | Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50=33 nM | 21341674 | ||
| human lung cancer cell line (H128) | Cytotoxic assay | In Vitro cytotoxicity against human lung cancer cell line (H128), IC50=31 nM | 11334569 | ||
| human HCT116 cells | Growth inhibition assay | Growth inhibition of human HCT116 cells by five-dose growth inhibition assay, GI50=30 nM | 25909279 | ||
| UACC 62 cells | Cytotoxic assay | Tested in vitro for cytotoxicity against human tumor cell line UACC 62 (melanoma), GI50=30 nM | 10714502 | ||
| HeLa cells | Growth inhibition assay | Growth inhibition of HeLa cells after 4 days, GI50=30 nM | 17418582 | ||
| SK-BR-3 cells | Cytotoxic assay | In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3), IC50=26 nM | 11334569 | ||
| 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 | ||
| human RPMI8226 cells | Cytotoxic assay | Cytotoxicity against human RPMI8226 cells by MTT method, IC50=21 nM | 19012996 | ||
| human SN12C cells | Growth inhibition assay | Growth inhibition of human SN12C cells by five-dose growth inhibition assay, GI50=20 nM | 25909279 | ||
| RPM18402 tumor cell line | Proliferation assay | Concentration required to inhibit cell proliferation in RPM18402 tumor cell line, IC50=20 nM | 15482929 | ||
| 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 | ||
| human HL60 cells | Function assay | Antitumor activity against human HL60 cells by SRB method, IC50=12 nM | 19541483 | ||
| LoVo cell line | Cytotoxic assay | Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line, IC50=11.6 nM | 12408707 | ||
| human lymphoblast tumor cell line RPM18402 | Cytotoxic assay | Cytotoxicity against human lymphoblast tumor cell line RPM18402, IC50=12 nM | 12392745 | ||
| human DU145 cells | Growth inhibition assay | Growth inhibition of human DU145 cells by five-dose growth inhibition assay, IC50=10 nM | 25909279 | ||
| human UACC62 cells | Growth inhibition assay | Growth inhibition of human UACC62 cells by five-dose growth inhibition assay, IC50=10 nM | 25909279 | ||
| human MCF7 cells | Growth inhibition assay | Growth inhibition of human MCF7 cells by five-dose growth inhibition assay, IC50=10 nM | 25909279 | ||
| human HOP62 cells | Growth inhibition assay | Growth inhibition of human HOP62 cells by five-dose growth inhibition assay, IC50=10 nM | 25909279 | ||
| LOX cells | Cytotoxic assay | Cytotoxicity was determined in vitro in LOX cells (melanoma) of human tumor cell lines by using MTT assay, IC50=5 nM | 7853331 | ||
| human colon carcinoma SW620 cell | Cytotoxic assay | Cytotoxic potentiation of Topotecan (TP) by the compound in human colon carcinoma SW620 cell line, IC50=3.2 nM | 12408707 | ||
| human colon cancer cell line (WiDr) | Cytotoxic assay | In Vitro cytotoxicity against human colon cancer cell line (WiDr), IC50=56 nM | 11334569 | ||
| MDA-MB-231 | Apoptosis assay | Induction of apoptosis in human MDA-MB-231 cells assessed as p53 phosphorylation at Ser15 by Western blotting analysis | 24980118 | ||
| A375 | Apoptosis assay | Induction of apoptosis in human A375 cells assessed as p53 phosphorylation at Ser15 by Western blotting analysis | 24980118 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | ||
| Daoy | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Topotecan HCl是一种拓扑异构酶I抑制剂，作用于MCF-7 Luc细胞和DU-145 Luc细胞，无细胞试验中IC50分别为13 nM和2 nM。Topotecan HCl 可诱导自噬和凋亡。 | ||||
|---|---|---|---|---|---|
| 特性 | Topotecan是camptothecin的水溶性衍生物。 | ||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Topotecan对DU-145 Luc和MCF-7 Luc细胞具有很强的药物活性。[1] DNA复制期间，Topotecan通过稳定拓扑异构酶I和DNA之间的共价复合物，并防止酶联单链DNA断裂后再连接，引起细胞毒性。在耐辐射的人B系急性淋巴细胞性白血病(ALL)细胞中，Topotecan稳定拓扑异构酶I/DNA可裂解复合物，尽管bcl-2高度表达，也能够引起快速的细胞凋亡，并且剂量依赖性抑制ALL细胞的克隆生长。 [2] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | MCF-7 Luc 和 DU-145 Luc 细胞 | ||
| 浓度 | 0 μg/mL - 0.692 μg/mL | |||
| 孵育时间 | 96小时 | |||
| 方法 | Topotecan溶解在无菌水中，物料浓度为1 mg/mL，在培养基中稀释为6 μg/mL，然后在不透明的，白色的，组织培养物处理的微孔板中以1:4连续稀释至0.1 mL/孔的终体积。MCF-7 Luc 和 DU-145 Luc细胞以3×104细胞/mL重悬浮在包含10% FBS和0.5 mg/mL Geneticin的高浓度葡萄糖DMEM中；每孔中加入100 μL细胞。板在37 °C，95% 湿度/5% CO2环境中培养4天。培养后，0.05 mL包含50 μg/mL D-荧光素的0.1 M HEPES 缓冲液(pH 7.9)加入到每个孔中。室温下培养10分钟后，培养微孔板在微孔板光度计和分子光成像仪上测量。微孔板光度计得到的结果使用不包含外源性药物的无抑制对照孔和包含ATP抑制剂的最大抑制对照孔进行计算。分子光成像法得到的结果使用5分钟发光成像得到的值类似计算。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | LC3 / p62 p53 / sesn2 / p-AMPK |
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23024792 | |
| Growth inhibition assay | Cell viability |
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28544814 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 皮下接种DU-145 Luc细胞的动物肿瘤模型中，通过尾铗和发光成像测定，Topotecan处理导致肿瘤消退。未处理的对照组相关系数为0.75，Topotecan处理组为0.93。同样，对于未治疗的和Topotecan治疗的腹腔注射移植MCF-7 Luc细胞的小鼠，肿瘤的发展与退化可使用发光成像检测。[1]在严重联合免疫缺陷(SCID)的人预后不良ALL小鼠模型中，Topotecan诱发有效的抗白血病活性。Topotecan全身药物暴露时，显著增加致命剂量人白血病细胞攻击的SCID小鼠的无病生存期。[2]神经胶质瘤优先表达TRAIL R2，用Topotecan治疗显著上调其表达。[3] |
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|---|---|---|
| 动物实验 | Animal Models | 负荷MCF-7 Luc 或 DU-145 Luc细胞的小鼠 |
| Dosages | 0.25 mg/mL | |
| Administration | 腹腔注射给药 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04455139 | Terminated | Eye Cancer Retinoblastoma |
Prof. Beck Popovic Maja|University of Lausanne Hospitals |
November 15 2021 | Phase 2 |
| NCT05083000 | Unknown status | COVID-19 Respiratory Infection |
National University Hospital Singapore|Christian Medical College Vellore India |
August 16 2021 | Phase 1 |
| NCT04156347 | Active not recruiting | Retinoblastoma |
Targeted Therapy Technologies LLC |
June 16 2021 | Phase 1 |
| NCT04428879 | Recruiting | Retinoblastoma |
The Hospital for Sick Children |
June 16 2020 | Phase 1 |
化学信息&溶解度
| 分子量 | 457.91 | 分子式 | C23H23N3O5.HCl |
| CAS号 | 119413-54-6 | SDF | Download Topotecan HCl SDF |
| Smiles | CCC1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC(=C5CN(C)C)O)N=C4C3=C2)O.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 91 mg/mL ( (198.72 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 91 mg/mL (198.72 mM) Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
I would like get the compound for mice intraperitoneally injection, What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?
回答：
Topotecan HCl is generally prepared by Saline for I.P. administration.
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