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別名: 6-MP 中文名稱:巰嘌呤
Mercaptopurine (6-MP)是一種廣泛應用于治療白血病的藥物,也是一種免疫抑制藥,通過整合巰基嘌呤的甲基轉(zhuǎn)移酶代謝產(chǎn)物進入DNA和RNA抑制新創(chuàng)嘌呤合成。
Mercaptopurine (6-MP) Chemical Structure
CAS: 50-44-2


| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| mouse J774.A1 cells | Proliferation assay | 3 days | Antiproliferative activity against mouse J774.A1 cells after 3 days by MTT conversion assay, IC50=0.003 μM | ||
| HEK293 cells | Proliferation assay | 3 days | Antiproliferative activity against HEK293 cells after 3 days by MTT conversion assay, IC50=0.007 μM | ||
| mouse J774 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse J774 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.003 μM | ||
| human PBMC | Function assay | 4 days | Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days, IC50=0.1495 μM | ||
| HeLa cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay, IC50=2.9 μM | ||
| A549 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay, IC50=47 μM | ||
| MCF7 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay, IC50=1.4 μM | ||
| MT4 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human MT4 cells infected with HTLV-1 after 96 hrs by MTT assay, CC50=0.1 μM | ||
| CCRF-CEM cells | Proliferation assay | 96 h | Antiproliferative activity against human CCRF-CEM cells after 96 hrs by MTT assay, CC50=1 μM | ||
| WIL2-NS cells | Proliferation assay | 96 h | Antiproliferative activity against human WIL2-NS cells after 96 hrs by MTT assay, CC50=3 μM | ||
| CCRF-SB cells | Proliferation assay | 96 h | Antiproliferative activity against human CCRF-SB cells after 96 hrs by MTT assay, CC50=1.1 μM | ||
| human DU145 cells | Proliferation assay | 96 h | Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, CC50=2 μM | ||
| human HepG2 cells | Proliferation assay | 96 h | Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, CC50=8 μM | ||
| MCF7 cells | Proliferation assay | 96 h | Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, CC50=3.2 μM | ||
| SK-MEL-28 cells | Proliferation assay | 96 h | Antiproliferative activity against human SK-MEL-28 cells after 96 hrs by MTT assay, CC50=15 μM | ||
| mouse S49 cells | Cytotoxicity assay | 72 h | Cytotoxicity against wild type mouse S49 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay, EC50=8 μM | ||
| A549 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=47 μM | ||
| MCF7 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50=1.4 μM | ||
| HeLa cells | Cytotoxicity assay | 48 h | Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50=2.9 μM | ||
| WEHI164 cells | Proliferation assay | 3 days | Antiproliferative activity against mouse WEHI164 cells after 3 days by MTT conversion assay, IC50=0.015 μM | ||
| WEHI164 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse WEHI164 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.017 μM | ||
| L1210 leukemia cells | Function assay | Inhibitory concentration on multidrug-resistant L1210 leukemia cells, IC50=0.024 μM | |||
| MT4 cells | Proliferation assay | Antiproliferative activity against human MT4 cells by MTT assay, IC50=0.1 μM | |||
| human CCRF-CEM cells | Proliferation assay | Antiproliferative activity against human CCRF-CEM cells by MTT assay, IC50=1 μM | |||
| human CCRF-SB cells | Proliferation assay | Antiproliferative activity against human CCRF-SB cells by MTT assay, IC50=1 μM | |||
| human SK-MEL-28 cells | Proliferation assay | Antiproliferative activity against human SK-MEL-28 cells by MTT assay, IC50=15 μM | |||
| human MCF7 cells | Proliferation assay | Antiproliferative activity against human MCF7 cells by MTT assay, IC50=3 μM | |||
| human HepG2 cells | Proliferation assay | Antiproliferative activity against human HepG2 cells by MTT assay, IC50=8 μM | |||
| human DU145 cells | Proliferation assay | Antiproliferative activity against human DU145 cells by MTT assay, IC50=2 μM | |||
| MCF7 cells | Cytotoxicity assay | Cytotoxicity against human MCF7 cells, IC50=2.79 μM | |||
| Colo-357 cells | Cytotoxicity assay | Cytotoxicity against human Colo-357 cells by crystal violet staining, IC50=6.12 μM | |||
| Aspc-1 cells | Cytotoxicity assay | Cytotoxicity against human Aspc-1 cells by crystal violet staining, IC50=2.45 μM | |||
| Patu-02 cells | Cytotoxicity assay | Cytotoxicity against human Patu-02 cells by crystal violet staining, IC50=9.69 μM | |||
| Patu-T cells | Cytotoxicity assay | Cytotoxicity against human Patu-T cells by crystal violet staining, IC50=4.09 μM | |||
| Patu-S cells | Cytotoxicity assay | Cytotoxicity against human Patu-S cells by crystal violet staining, IC50=11.07 μM | |||
| T3M4 cells | Cytotoxicity assay | Cytotoxicity against human T3M4 cells by crystal violet staining, IC50=2.63 μM | |||
| human PANC1 cells | Cytotoxicity assay | Cytotoxicity against human PANC1 cells by crystal violet staining, IC50=6.39 μM | |||
| human DAN-G cells | Cytotoxicity assay | Cytotoxicity against human DAN-G cells by crystal violet staining, IC50=4.06 μM | |||
| WIL-2NS cells | Proliferation assay | Antiproliferative activity against human WIL-2NS cells by MTT assay, IC50=3 μM | |||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
| 產(chǎn)品描述 | Mercaptopurine (6-MP)是一種廣泛應用于治療白血病的藥物,也是一種免疫抑制藥,通過整合巰基嘌呤的甲基轉(zhuǎn)移酶代謝產(chǎn)物進入DNA和RNA抑制新創(chuàng)嘌呤合成。 | |
|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | Mercaptopurine被廣泛用于治療惡性腫瘤,風濕性疾病,皮膚病,炎癥性腸道疾病,以及實體器官移植排斥。 Mercaptopurine通過抑制磷酸核糖焦磷酸酰胺轉(zhuǎn)移酶(PRPP酰胺轉(zhuǎn)移酶)而抑制嘌呤核苷和代謝。PRPP酰胺轉(zhuǎn)移酶是嘌呤合成的限速酶。它會改變RNA和DNA的合成和功能。Mercaptopurine干擾核苷酸的互變和糖蛋白的合成。 |
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|---|---|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04770922 | Completed | Acute Lymphoblastic Leukemia Pediatric|Adverse Drug Event |
Cipherome Inc.|Stanford University |
February 23 2021 | -- |
| NCT03022747 | Unknown status | Lymphoblastic Leukemia Acute Childhood |
Vastra Gotaland Region |
January 2017 | Phase 2 |
|
| 分子量 | 152.18 | 分子式 | C5H4N4S |
| CAS號 | 50-44-2 | SDF | Download Mercaptopurine (6-MP) SDF |
| Smiles | C1=NC2=C(N1)C(=S)N=CN2 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 30 mg/mL ( (197.13 mM) ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解配方 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 | |||||
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)
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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