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Topotecan HCl

別名: Nogitecan HCl, SKFS 104864A, NSC 609699 中文名稱(chēng)：鹽酸托泊替康

Topotecan HCl是一種拓?fù)洚悩?gòu)酶I抑制劑，作用于MCF-7 Luc細(xì)胞和DU-145 Luc細(xì)胞，無(wú)細(xì)胞試驗(yàn)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

Topotecan HCl Chemical Structure

CAS: 119413-54-6

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 1872.81 現(xiàn)貨
50mg 1466.89 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Topotecan HCl相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Topoisomerase Signaling Pathways

Topoisomerase信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類(lèi)型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Topotecan HCl是一種拓?fù)洚悩?gòu)酶I抑制劑，作用于MCF-7 Luc細(xì)胞和DU-145 Luc細(xì)胞，無(wú)細(xì)胞試驗(yàn)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(diǎn)
Topo I (DU-145 Luc cells) [1]
(Cell-free assay)		 Topo I (MCF-7 Luc cells) [1]
(Cell-free assay)
2 nM 13 nM
體外研究(In Vitro)
體外研究活性

Topotecan對(duì)DU-145 Luc和MCF-7 Luc細(xì)胞具有很強(qiáng)的藥物活性。[1] DNA復(fù)制期間，Topotecan通過(guò)穩(wěn)定拓?fù)洚悩?gòu)酶I和DNA之間的共價(jià)復(fù)合物，并防止酶聯(lián)單鏈DNA斷裂后再連接，引起細(xì)胞毒性。在耐輻射的人B系急性淋巴細(xì)胞性白血病(ALL)細(xì)胞中，Topotecan穩(wěn)定拓?fù)洚悩?gòu)酶I/DNA可裂解復(fù)合物，盡管bcl-2高度表達(dá)，也能夠引起快速的細(xì)胞凋亡，并且劑量依賴(lài)性抑制ALL細(xì)胞的克隆生長(zhǎng)。 [2]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MCF-7 Luc 和 DU-145 Luc 細(xì)胞
濃度 0 μg/mL - 0.692 μg/mL
孵育時(shí)間 96小時(shí)
方法

Topotecan溶解在無(wú)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(xì)胞以3×104細(xì)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(xì)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(gè)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(jì)和分子光成像儀上測(cè)量。微孔板光度計(jì)得到的結(jié)果使用不包含外源性藥物的無(wú)抑制對(duì)照孔和包含ATP抑制劑的最大抑制對(duì)照孔進(jìn)行計(jì)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(lèi)似計(jì)算。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)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(xì)胞的動(dòng)物腫瘤模型中，通過(guò)尾鋏和發(fā)光成像測(cè)定，Topotecan處理導(dǎo)致腫瘤消退。未處理的對(duì)照組相關(guān)系數(shù)為0.75，Topotecan處理組為0.93。同樣，對(duì)于未治療的和Topotecan治療的腹腔注射移植MCF-7 Luc細(xì)胞的小鼠，腫瘤的發(fā)展與退化可使用發(fā)光成像檢測(cè)。[1]在嚴(yán)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(shí)，顯著增加致命劑量人白血病細(xì)胞攻擊的SCID小鼠的無(wú)病生存期。[2]神經(jīng)膠質(zhì)瘤優(yōu)先表達(dá)TRAIL R2，用Topotecan治療顯著上調(diào)其表達(dá)。[3]
動(dòng)物實(shí)驗(yàn) Animal Models 負(fù)荷MCF-7 Luc 或 DU-145 Luc細(xì)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(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 91 mg/mL ( (198.72 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : 91 mg/mL (198.72 mM)

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(jìn)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(jiàn)問(wèn)題及建議解決方法

問(wèn)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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