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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
相關(guān)靶點 | WNT β-catenin Wnt/β-catenin | 點擊展開 |
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相關(guān)產(chǎn)品 | IWR-1-endo IWP-2 SKL2001 BML-284 (Wnt agonist 1) PRI-724 FH535 PNU-74654 LF3 KYA1797K KY02111 iCRT3 Adavivint (SM04690) MSAB Isoquercitrin IQ-1 iCRT14 CCT251545 Isoxazole 9 (ISX-9) JW55 Methyl Vanillate M435-1279 WAY-262611 JW74 | 點擊展開 |
相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 干細胞小分子化合物庫 GPCR小分子化合物庫 干細胞分化化合物庫 | 點擊展開 |
細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
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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 | ||
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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。 | |
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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(zhuǎn)運體ABC(ATP結(jié)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(zhì)中K+外流、并抑制氧化磷酸化。Salinomycin能夠誘導(dǎo)不同起源的人類癌細胞系的大量凋亡[1]。 | |||
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細胞實驗 | 細胞系 | 結(jié)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。 |
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(dǎo)預(yù)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(jié)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(dǎo)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(dǎo)致腫瘤轉(zhuǎn)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]。 | |
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動物實驗 | Animal Models | NOD/SCID小鼠 |
Dosages | 5 mg/kg | |
Administration | 腹腔注射 |
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) | |||
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 |
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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 |
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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)
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)
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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