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DNA Damage/DNA Repair
Topoisomerase inhibitor
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Apoptosis related activator
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Autophagy activator
Topotecan HCl
僅限科研使用
Topotecan HCl
別名: Nogitecan HCl, SKFS 104864A, NSC 609699 中文名稱：鹽酸托泊替康
Topotecan HCl是一種拓撲異構(gòu)酶I抑制劑，作用于MCF-7 Luc細胞和DU-145 Luc細胞，無細胞試驗中IC50分別為13 nM和2 nM。Topotecan HCl 可誘導(dǎo)自噬和凋亡。
Topotecan HCl Chemical Structure
CAS: 119413-54-6
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
Topotecan HCl相關(guān)產(chǎn)品
| 相關(guān)靶點 | Topo I Topo II Topo IV | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan | 點擊展開 |
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 凋亡分子化合物庫 DNA損傷/ DNA修復(fù)化合物庫 細胞周期化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Topotecan HCl是一種拓撲異構(gòu)酶I抑制劑，作用于MCF-7 Luc細胞和DU-145 Luc細胞，無細胞試驗中IC50分別為13 nM和2 nM。Topotecan HCl 可誘導(dǎo)自噬和凋亡。 | ||||
|---|---|---|---|---|---|
| 特性 | Topotecan是camptothecin的水溶性衍生物。 | ||||
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Topotecan對DU-145 Luc和MCF-7 Luc細胞具有很強的藥物活性。[1] DNA復(fù)制期間，Topotecan通過穩(wěn)定拓撲異構(gòu)酶I和DNA之間的共價復(fù)合物，并防止酶聯(lián)單鏈DNA斷裂后再連接，引起細胞毒性。在耐輻射的人B系急性淋巴細胞性白血病(ALL)細胞中，Topotecan穩(wěn)定拓撲異構(gòu)酶I/DNA可裂解復(fù)合物，盡管bcl-2高度表達，也能夠引起快速的細胞凋亡，并且劑量依賴性抑制ALL細胞的克隆生長。 [2] |
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|---|---|---|---|---|
| 細胞實驗 | 細胞系 | MCF-7 Luc 和 DU-145 Luc 細胞 | ||
| 濃度 | 0 μg/mL - 0.692 μg/mL | |||
| 孵育時間 | 96小時 | |||
| 方法 | Topotecan溶解在無菌水中，物料濃度為1 mg/mL，在培養(yǎng)基中稀釋為6 μg/mL，然后在不透明的，白色的，組織培養(yǎng)物處理的微孔板中以1:4連續(xù)稀釋至0.1 mL/孔的終體積。MCF-7 Luc 和 DU-145 Luc細胞以3×104細胞/mL重懸浮在包含10% FBS和0.5 mg/mL Geneticin的高濃度葡萄糖DMEM中；每孔中加入100 μL細胞。板在37 °C，95% 濕度/5% CO2環(huán)境中培養(yǎng)4天。培養(yǎng)后，0.05 mL包含50 μg/mL D-熒光素的0.1 M HEPES 緩沖液(pH 7.9)加入到每個孔中。室溫下培養(yǎng)10分鐘后，培養(yǎng)微孔板在微孔板光度計和分子光成像儀上測量。微孔板光度計得到的結(jié)果使用不包含外源性藥物的無抑制對照孔和包含ATP抑制劑的最大抑制對照孔進行計算。分子光成像法得到的結(jié)果使用5分鐘發(fā)光成像得到的值類似計算。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | LC3 / p62 p53 / sesn2 / p-AMPK |
|
23024792 | |
| Growth inhibition assay | Cell viability |
|
28544814 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 皮下接種DU-145 Luc細胞的動物腫瘤模型中，通過尾鋏和發(fā)光成像測定，Topotecan處理導(dǎo)致腫瘤消退。未處理的對照組相關(guān)系數(shù)為0.75，Topotecan處理組為0.93。同樣，對于未治療的和Topotecan治療的腹腔注射移植MCF-7 Luc細胞的小鼠，腫瘤的發(fā)展與退化可使用發(fā)光成像檢測。[1]在嚴重聯(lián)合免疫缺陷(SCID)的人預(yù)后不良ALL小鼠模型中，Topotecan誘發(fā)有效的抗白血病活性。Topotecan全身藥物暴露時，顯著增加致命劑量人白血病細胞攻擊的SCID小鼠的無病生存期。[2]神經(jīng)膠質(zhì)瘤優(yōu)先表達TRAIL R2，用Topotecan治療顯著上調(diào)其表達。[3] |
|
|---|---|---|
| 動物實驗 | Animal Models | 負荷MCF-7 Luc 或 DU-145 Luc細胞的小鼠 |
| Dosages | 0.25 mg/mL | |
| Administration | 腹腔注射給藥 | |
| 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 |
化學(xué)信息&溶解度
| 分子量 | 457.91 | 分子式 | C23H23N3O5.HCl |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 91 mg/mL ( (198.72 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : 91 mg/mL (198.72 mM) Ethanol : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 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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