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Salinomycin (from Streptomyces albus)
別名: Procoxacin 中文名稱：鹽霉素（來自白色鏈霉菌）
Salinomycin (Procoxacin), 曾經(jīng)被用作抗球蟲藥，具有抗癌和抗腫瘤干細胞的效果。
Salinomycin (from Streptomyces albus) Chemical Structure
CAS: 53003-10-4
產(chǎn)品質控
Salinomycin (from Streptomyces albus)相關產(chǎn)品
相關信號通路圖
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 |
|---|---|---|---|---|---|
| BT474 | Function assay | 7.5 uM | 3 days | Disruption of preformed spheroids in human BT474 cancer stem cells at 7.5 uM after 3 days by microscopic analysis | ChEMBL |
| DU145 | Function assay | 7.5 uM | 3 days | Disruption of preformed spheroids in human DU145 cancer stem cells at 7.5 uM after 3 days by microscopic analysis | ChEMBL |
| HT-29 cells | Proliferation assay | 72 h | Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.03 μM | 25644674 | |
| LS180 cells | Proliferation assay | 72 h | Antiproliferative activity against human LS180 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=0.61 μM | 25644674 | |
| LoVo cells | Proliferation assay | 72 h | Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50=0.36 μM | 25644674 | |
| MV4-11 cells | Proliferation assay | 72 h | Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50=0.33 μM | 26163197 | |
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.29 μM | 25644674 | |
| SW707 cells | Proliferation assay | 72 h | Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=1.73 μM | 25644674 | |
| HL60/Vinc cells | Cytotoxicity assay | 72 h | Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50=3.44 μM | 23079523 | |
| BALB/3T3 cells | Cytotoxicity assay | 72 h | Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50=28.08 μM | 23079523 | |
| HL60 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HL60 cells incubated for 72 hrs by MTT assay, IC50 = 0.44 μM. | 23079523 | |
| LoVo | Cytotoxicity assay | 72 hrs | Cytotoxicity against human LoVo cells incubated for 72 hrs by MTT assay, IC50 = 1.11 μM. | 23079523 | |
| HL60/Vinc | Cytotoxicity assay | 72 hrs | Cytotoxicity against vincristine-resistant human HL60/Vinc cells incubated for 72 hrs by MTT assay, IC50 = 3.44 μM. | 23079523 | |
| LoVo/DX | Cytotoxicity assay | 72 hrs | Cytotoxicity against doxorubicin-resistant human LoVo/DX cells incubated for 72 hrs by MTT assay, IC50 = 6.23 μM. | 23079523 | |
| BALB/3T3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BALB/3T3 cells incubated for 72 hrs by MTT assay, IC50 = 28.08 μM. | 23079523 | |
| HL60 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 0.29 μM. | 25644674 | |
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.36 μM. | 25644674 | |
| LS180 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LS180 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.61 μM. | 25644674 | |
| LoVo/DX | Antiproliferative assay | 72 hrs | Antiproliferative activity against human doxorubicin-resistant LoVo/DX cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 0.76 μM. | 25644674 | |
| HT-29 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 1.03 μM. | 25644674 | |
| SW707 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 1.73 μM. | 25644674 | |
| HL60/Vinc | Antiproliferative assay | 72 hrs | Antiproliferative activity against human vincristine-resistant HL60/Vinc cells assessed as growth inhibition after 72 hrs by MTT assay, IC50 = 2.09 μM. | 25644674 | |
| BALB/3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method, IC50 = 9.33 μM. | 25644674 | |
| MV4-11 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50 = 0.33 μM. | 26163197 | |
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells after 72 hrs, IC50 = 0.53 μM. | 26163197 | |
| LoVo/DX | Antiproliferative assay | 72 hrs | Antiproliferative activity against doxorubicin-resistant human LoVo/DX cells after 72 hrs, IC50 = 0.59 μM. | 26163197 | |
| BALB/3T3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BALB/3T3 cells after 72 hrs, IC50 = 27.76 μM. | 26163197 | |
| JIMT1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human JIMT1 cells after 72 hrs by MTT assay, IC50 = 0.52 μM. | 27326340 | |
| MCF7 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.59 μM. | 27326340 | |
| MCF7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 2.98 μM. | 27876192 | |
| MDA-MB-231 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 6.42 μM. | 27876192 | |
| MIAPaCa2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | |
| DU145 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human DU145 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | |
| BT474 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT474 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 48 hrs by MTS assay | 28177244 | |
| HT-29 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HT-29 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 1.43 μM. | 28262526 | |
| HGC27 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HGC27 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 2.57 μM. | 28262526 | |
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell proliferation after 48 hrs by MTT assay, IC50 = 6.53 μM. | 28262526 | |
| OV2008 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 3.2 μM. | 28651817 | |
| OV2008 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50 = 4.78 μM. | 28651817 | |
| OV2008 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human OV2008 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay, IC50 = 7.44 μM. | 28651817 | |
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 1.43 μM. | 28688275 | |
| HEK293 | Cytotoxicity assay | 72 hrs | Cytotoxicity against HEK293 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.195 μM. | 29466777 | |
| HEK293 | Cytotoxicity assay | 72 hrs | Cytotoxicity against doxycycline inducible T-Rex/K-Ras G12V HEK293 cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 0.3295 μM. | 29466777 | |
| HL60 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 0.58 μM. | 29466777 | |
| SW480 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SW480 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.77 μM. | 29466777 | |
| 4T1 | Cytotoxicity assay | 48 hrs | Cytotoxicity against mouse 4T1 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.78 μM. | 29466777 | |
| A549 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 3.98 μM. | 29466777 | |
| HeLa | Cytotoxicity assay | 48 hrs | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 4.49 μM. | 29466777 | |
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 9.08 μM. | 29466777 | |
| SMMC7721 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 12.04 μM. | 29466777 | |
| BEAS2B | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BEAS2B cells assessed as cell growth inhibition after 48 hrs by MTS assay, IC50 = 13.07 μM. | 29466777 | |
| LoVo | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo cells after 72 hrs by SRB assay, IC50 = 0.44 μM. | 30025346 | |
| LoVo/DX | Antiproliferative assay | 72 hrs | Antiproliferative activity against human LoVo/DX cells after 72 hrs by SRB assay, IC50 = 0.69 μM. | 30025346 | |
| SK-BR-3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SK-BR-3 cells after 72 hrs by SRB assay, IC50 = 0.89 μM. | 30025346 | |
| JIMT1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human JIMT1 cells after 72 hrs by SRB assay, IC50 = 1.3 μM. | 30025346 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 1.5 μM. | 30025346 | |
| ALL5 | Antiproliferative assay | 120 hrs | Antiproliferative activity against human ALL5 cells after 120 hrs by MTT assay, IC50 = 2.4 μM. | 30025346 | |
| MCF10A | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF10A cells after 72 hrs by SRB assay, IC50 = 46 μM. | 30025346 | |
| HT-29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 3.21 μM. | 30684870 | |
| HGC27 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HGC27 cells after 48 hrs by MTT assay, IC50 = 8.18 μM. | 30684870 | |
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay, IC50 = 24.5 μM. | 30871771 | |
| HL60 | Cytotoxicity assay | 24 hrs | Cytotoxicity against human HL60 cells assessed as growth inhibition after 24 hrs by resazurin dye based assay, GI50 = 6.63 μM. | 30986574 | |
| HL-60 | Function assay | 24 hrs | Trypanocidal activity against bloodstream forms of Trypanosoma brucei infected in human HL-60 cells incubated for 24 hrs followed by compound wash out after 72 hrs, GI50 = 0.18 μM. | 31103901 | |
| MDCK | Antiviral assay | 3 days | Antiviral activity against Influenza A virus (A/Hong Kong/7/1987(H3N2)) infected in MDCK cells after 3 days by MTT assay, EC50 = 0.4 μM. | 31103901 | |
| Vero | Antiviral assay | 24 hrs | Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr, IC50 = 0.24 μM. | ChEMBL | |
| MIAPaCa2 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTS assay, CC50 = 6.5 μM. | ChEMBL | |
| BT474 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human BT474 cells after 48 hrs by MTS assay, CC50 = 14 μM. | ChEMBL | |
| VCaP cells | Proliferation assay | Antiproliferative activity against human VCaP cells, EC50=0.38 μM | 23063400 | ||
| VCaP | Antiproliferative assay | Antiproliferative activity against human VCaP cells, EC50 = 0.38 μM. | 23063400 | ||
| LoVo/DX | Antiproliferative assay | Antiproliferative activity against human LoVo/DX cells, IC50 = 1 μM. | 24631190 | ||
| HL60 | Antiproliferative assay | Antiproliferative activity against human HL60 cells, IC50 = 1.2 μM. | 24631190 | ||
| LoVo | Antiproliferative assay | Antiproliferative activity against human LoVo cells, IC50 = 1.5 μM. | 24631190 | ||
| HL60/Vinc | Antiproliferative assay | Antiproliferative activity against human HL60/Vinc cells, IC50 = 4.7 μM. | 24631190 | ||
| BALB/3T3 | Antiproliferative assay | Antiproliferative activity mouse BALB/3T3 cells, IC50 = 25.8 μM. | 24631190 | ||
| HMLER | Antiproliferative assay | Antiproliferative activity against HMLER cells by MTT assay Breast cancer stem cell, IC50 = 0.1 μM. | 30684870 | ||
| HeLa | Antiproliferative assay | Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 0.32 μM. | 30684870 | ||
| LoVo | Antiproliferative assay | Antiproliferative activity against human LoVo cells by SRB assay, IC50 = 0.44 μM. | 30684870 | ||
| JIMT1 | Antiproliferative assay | Antiproliferative activity against human JIMT1 cells, IC50 = 0.52 μM. | 30684870 | ||
| JIMT1 | Antiproliferative assay | Antiproliferative activity against human JIMT1 cells by MTT assay, IC50 = 0.52 μM. | 30684870 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 0.59 μM. | 30684870 | ||
| LoVo/DX | Antiproliferative assay | Antiproliferative activity against human LoVo/DX cells by SRB assay, IC50 = 0.69 μM. | 30684870 | ||
| SKBR3 | Antiproliferative assay | Antiproliferative activity against human SKBR3 cells by SRB assay, IC50 = 0.89 μM. | 30684870 | ||
| HT-29 | Antiproliferative assay | Antiproliferative activity against human HT-29 cells by MTT assay, IC50 = 1.03 μM. | 30684870 | ||
| JIMT1 | Antiproliferative assay | Antiproliferative activity against human JIMT1 cells by SRB assay, IC50 = 1.3 μM. | 30684870 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells by SRB assay, IC50 = 1.5 μM. | 30684870 | ||
| HGC27 | Antiproliferative assay | Antiproliferative activity against human HGC27 cells by MTT assay, IC50 = 2.57 μM. | 30684870 | ||
| 4T1 | Antiproliferative assay | Antiproliferative activity against mouse 4T1 cells by MTT assay, IC50 = 3.78 μM. | 30684870 | ||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells by MTT assay, IC50 = 3.98 μM. | 30684870 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells by SRB assay, IC50 = 6.42 μM. | 30684870 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells by MTT assay, IC50 = 6.91 μM. | 30684870 | ||
| Caco2 | Antiproliferative assay | Antiproliferative activity against human Caco2 cells by MTT assay, IC50 = 12.99 μM. | 30684870 | ||
| U87 | Antiproliferative assay | Antiproliferative activity against human U87 cells by MTT assay, IC50 = 38.7 μM. | 30684870 | ||
| MCF10A | Antiproliferative assay | Antiproliferative activity against human MCF10A cells by SRB assay, IC50 = 46 μM. | 30684870 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Salinomycin (Procoxacin), 曾經(jīng)被用作抗球蟲藥，具有抗癌和抗腫瘤干細胞的效果。 | |
|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | Salinomycin是一種從Streptomyces albus中分離的聚醚類離子載體型抗生素，通過干擾藥物轉運體ABC（ATP結合位點）、Wnt/β-catenin及其他CSC信號通路，在多種不同的人類癌癥中，殺死癌癥干細胞。Salinomycin對Gram陽性的細菌具有抗菌活性，除此之外，salinomycin在不同的生物膜中發(fā)揮作用，包括胞膜、線粒體膜，其作為單價陽離子載體，對堿金屬離子有較強的選擇性，對K+有偏好性，因此能促進線粒體和胞質中K+外流、并抑制氧化磷酸化。Salinomycin能夠誘導不同起源的人類癌細胞系的大量凋亡[1]。 | |||
|---|---|---|---|---|
| 細胞實驗 | 細胞系 | 結腸癌細胞(SW480, SW620, RKO)、乳腺癌細胞系(MCF-7, T47D, MDA-MB-453). | ||
| 濃度 | 1, 2.5, 5, 10 μM | |||
| 孵育時間 | 26 h | |||
| 方法 | 將細胞以1500/孔（SW480或SW620）或4000/孔（其他細胞系）的密度鋪于平底96孔板。16小時后，用salinomycin對細胞進行處理22小時，然后每孔加入溶于PBS中的5 mg/ml MTT，4小時，加入triplex solution裂解細胞。讀取562 nm出的吸光值。 |
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| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Salinomycin能夠有效地消除癌癥干細胞，從而誘導預處理過的和具有藥物抗性的癌癥部分臨床回歸。它還是陽性的離子型和變時型試劑，其處理過后能加大心輸出量、左心室收縮壓、提高心率、平均動脈壓、灌裝動脈血管舒張以及血流量、血漿兒茶酚胺的濃度。這些實驗結果都是以口服、吸入式注射150?μg/kg salinomycin的交交犬為模型進行的研究。然而，在哺乳動物中如馬、貓、豬和羊駝，salinomycin被報導在偶然的口服或吸入攝入的情況下，具有相當大的毒性作用。風險評估數(shù)據(jù)表明，人類可接受的salinomycin每日可攝入量為5 μg/kg，超過500 μg/kg的每日攝入量會對狗產(chǎn)生神經(jīng)毒性，如髓鞘損失、軸索變性。靜脈注射200-250 μg/kg的salinomycin三周（隔天注射）會導致腫瘤轉移的部分消退、僅有非常小的急性、長期副作用，使用傳統(tǒng)的化療藥物治療途徑，則沒有嚴重的急性長期副作用[1]。 | |
|---|---|---|
| 動物實驗 | Animal Models | NOD/SCID小鼠 |
| Dosages | 5 mg/kg | |
| Administration | 腹腔注射 | |
化學信息&溶解度
| 分子量 | 751.00 | 分子式 | C42H70O11 |
| CAS號 | 53003-10-4 | SDF | Download Salinomycin (from Streptomyces albus) SDF |
| Smiles | CCC(C1CCC(C(O1)C(C)C(C(C)C(=O)C(CC)C2C(CC(C3(O2)C=CC(C4(O3)CCC(O4)(C)C5CCC(C(O5)C)(CC)O)O)C)C)O)C)C(=O)O | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (133.15 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 100 mg/mL (133.15 mM) Water : Insoluble |
摩爾濃度計算器 |
|
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。
技術支持
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