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Salinomycin (Procoxacin) Wnt/beta-catenin 억제제

제품 번호S8129

Salinomycin은 전통적으로 항콕시듐 약물로 사용되어 왔으나, 최근 항암 및 항암 줄기세포(CSC) 효과를 나타내는 것으로 밝혀졌습니다.
Salinomycin (Procoxacin) Wnt/beta-catenin 억제제 Chemical Structure

화학 구조

분자량: 751.00

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품질 관리

배치: 순도: >97%
97

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
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
MV4-11 cells Proliferation assay 72 h Antiproliferative activity against human MV4-11 cells after 72 hrs, IC50=0.33 μM 26163197
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
VCaP cells Proliferation assay Antiproliferative activity against human VCaP cells, EC50=0.38 μM 23063400
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
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
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
VCaP Antiproliferative assay Antiproliferative activity against human VCaP cells, EC50 = 0.38 μM. 23063400
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
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
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
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
HT-29 Antiproliferative assay 48 hrs Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay, IC50 = 3.21 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
HGC27 Antiproliferative assay 48 hrs Antiproliferative activity against human HGC27 cells after 48 hrs by MTT assay, IC50 = 8.18 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
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
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 751.00 화학식

C42H70O11

보관 (수령일로부터)
CAS 번호 53003-10-4 SDF 다운로드 원액 보관

동의어 Procoxacin 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

용해도

In vitro
배치:

DMSO : 100 mg/mL (133.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC50/Ki
Wnt/β-catenin
시험관 내(In vitro)
Streptomyces albus에서 분리된 폴리에테르 이오노포어 항생제인 살리노마이신은 ABC(ATP-binding cassette) 약물 수송체, Wnt/beta-catenin 신호 경로 및 기타 CSC 경로를 방해하여 다양한 유형의 인간 암에서 CSC를 죽이는 것으로 나타났습니다. 이는 Bacillus subtilis, Staphylococcus aureus, Micrococcus flavus, Sarcina lutea, Mycobacterium spp., 일부 사상균류, Plasmodium falciparum 및 가금류 질병 콕시디움증을 유발하는 원생동물 기생충인 Eimeria spp.를 포함한 그람 양성균에 대한 항균 활성을 보입니다. 또한, 이 화합물은 이른 시기에 세포질 및 미토콘드리아 막을 포함한 다양한 생체막에서 단일가 양이온 이오노포어로 작용하며 알칼리 이온에 대한 엄격한 선택성과 K+에 대한 강한 선호도를 보여, 미토콘드리아 및 세포질 K+ 유출을 촉진하고 산화적 인산화를 억제하는 것으로 나타났습니다. 살리노마이신은 약물 및 세포자멸사 저항성의 여러 메커니즘을 나타내는 다양한 기원의 인간 암세포에서 대규모 세포자멸사를 유도할 수 있습니다.
생체 내(In vivo)
Salinomycin (from Streptomyces albus)은 CSC를 효과적으로 제거하고 심하게 전처리되고 치료 저항성인 암의 부분적인 임상적 퇴행을 유도할 수 있습니다. 또한 심장 박출량, 좌심실 수축기압, 심박수, 평균 동맥압, 관상동맥 혈관 확장 및 혈류, 혈장 카테콜아민 농도를 증가시키는 양성 이노트로픽 및 크로노트로픽 약물로도 입증되었습니다. 이러한 결과는 150 µg/kg의 이 화합물을 단일 정맥 주사받은 잡종견을 대상으로 한 실험에서 얻어졌습니다. 그러나 우발적인 경구 또는 흡입 섭취 후 말, 돼지, 고양이 및 알파카와 같은 포유류에서 살리노마이신의 상당한 독성이 보고되었습니다. 유럽 식품 안전청이 최근 발표한 위험 평가 데이터는 인간의 경우 5 µg/kg 살리노마이신의 일일 허용 섭취량(ADI)을 선언합니다. 이는 개가 500 µg/kg 이상의 살리노마이신을 매일 섭취하면 미엘린 손실 및 축삭 변성과 같은 신경독성 효과를 유발하기 때문입니다. 3주 동안 격일로 200-250 µg/kg 살리노마이신을 정맥 투여하면 종양 전이의 부분적인 퇴행을 초래하고 경미한 급성 및 장기 부작용만 나타나지만, 기존의 화학 요법 약물에서 관찰되는 심각한 급성 및 장기 부작용은 없습니다.
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