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Melphalan
别名: Alkeran, Sarcolysin, L-PAM 中文名称：米尔法兰
Melphalan (Alkeran, Sarcolysin, L-PAM)是氮芥的苯丙氨酸衍生物，具有抗肿瘤活性。此产品为危化品（急性毒性/易燃/皮肤腐蚀），请在穿戴防护面罩、防护手套和防护服后使用。 已取得危险化学品经营许可
Melphalan Chemical Structure
CAS: 148-82-3
产品质控
批次：
纯度：
99.47%
99.47
Melphalan相关产品
| 相关靶点 | AGT | 点击展开 |
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| 相关化合物库 | FDA药物库 天然产物库 凋亡分子化合物库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| K562 | Cytotoxicity assay | 1 h | In vitro cytotoxic activity against human leukemic cell line K562 after incubation for 1 hour, IC50=30 μM | ||
| L1210 cell | Cytotoxicity assay | 72 h | Tested in vitro for the cytotoxicity as number of viable cells against L1210 cell line after 72 hr treatment at conc. of 10E-6, ID50=1.7 μM | ||
| LoVo cell | Growth inhibition assay | 144 hr | Tested in vitro for inhibition after 144 hr exposure against human colon carcinoma LoVo cell line, IC50=4.09 μM | ||
| MOLT3 cells | Function assay | 72 h | Antitumor activity against human MOLT3 cells in presence of Penicillin-G-amidase after 72 hrs by XTT assay, IC50=0.3 μM | ||
| RT4 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human RT4 cells after 96 hrs by microtiter assay, IC50=14.25 μM | ||
| RT112 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human RT112 cells after 96 hrs by microtiter assay, IC50=4.69 μM | ||
| 5637 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human 5637 cells after 96 hrs by microtiter assay, IC50=0.31 μM | ||
| KYSE70 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human KYSE70 cells after 96 hrs by microtiter assay, IC50=16.16 μM | ||
| KYSE510 | Cytotoxicity assay | 96 h | Cytotoxicity against human KYSE510 cells after 96 hrs by microtiter assay, IC50=8.18 Μm | ||
| KYSE520 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human KYSE520 cells after 96 hrs by microtiter assay, IC50=10.49 μM | ||
| YAPC cells | Cytotoxicity assay | 96 h | Cytotoxicity against human YAPC cells after 96 hrs by microtiter assay, IC50=5.95 μM | ||
| DAN-G cells | Cytotoxicity assay | 96 h | Cytotoxicity against human DAN-G cells after 96 hrs by microtiter assay, IC50=2.65 μM | ||
| SISO cells | Cytotoxicity assay | 96 h | Cytotoxicity against human SISO cells after 96 hrs by microtiter assay, IC50=1 μM | ||
| LCLC-103H cells | Cytotoxicity assay | 96 h | Cytotoxicity against human LCLC-103H cells after 96 hrs by microtiter assay, IC50=4 μM | ||
| MCF7 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human MCF7 cells after 96 hrs by microtiter assay, IC50=3.71 μM | ||
| A427 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human A427 cells after 96 hrs by microtiter assay, IC50=5.13 μM | ||
| Caov3 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay | ||
| NSCLC cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human NSCLC cells assessed as cell growth after 48 hrs by SRB assay, GI50=6.736083 μM | ||
| CNSC cells | Cytotoxicity assay | 48 hrs | Cytotoxicity against human CNSC cells assessed as cell growth after 48 hrs by SRB assay, GI50=7.58578 μM | ||
| mouse FM3A/0 cells | Proliferation assay | 48 hrs | Antiproliferative activity against mouse FM3A/0 cells assessed as inhibition of cell growth after 48 hrs by ZF-Coulter Counting, IC50=3.6 μM | ||
| CEM/0 cells | Proliferation assay | 48 hrs | Antiproliferative activity against human CEM/0 cells assessed as inhibition of cell growth after 48 hrs by ZF-Coulter Counting, IC50=3.5 μM | ||
| HeLa cells | Proliferation assay | 48 hrs | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 48 hrs by ZF-Coulter Counting, IC5=1.9 μM | ||
| SH-SY5Y cells | Cytotoxicity assay | 72 h | Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay, IC50=5.5 μM | ||
| U251 cells | Cytotoxicity assay | 5 days | Cytotoxicity against human U251 cells after 5 days by MTT assay, IC50=3 μM | ||
| A549 cells | Cytotoxicity assay | 5 days | Cytotoxicity against human A549 cells after 5 days by MTT assay, IC50=3 μM | ||
| PANC1 cells | Cytotoxicity assay | 5 days | Cytotoxicity against human PANC1 cells after 5 days by MTT assay, IC50=3 μM | ||
| HT-29 cells | Cytotoxicity assay | 5 days | Cytotoxicity against human HT-29 cells after 5 days by MTT assay, IC50=3 μM | ||
| DLD1 cells | Cytotoxicity assay | 5 days | Cytotoxicity against human DLD1 cells after 5 days by MTT assay, IC50=3 μM | ||
| HeLa cells | Cytotoxicity assay | 4 days | Cytotoxicity against human HeLa cells after 4 days by Coulter counter analysis, IC50=1.9 μM | ||
| FM3A cells | Cytotoxicity assay | 2 days | Cytotoxicity against mouse FM3A cells after 2 days by Coulter counter analysis, IC50=3.6 μM | ||
| HL-60(TB) cells | Function assay | 24 h | Antileukemic activity against human HL-60(TB) cells assessed as inhibition of tumor growth after 24 hrs, IC50=0.38 μM | ||
| SR cells | Function assay | 24 h | Antileukemic activity against human SR cells assessed as inhibition of tumor growth after 24 hrs, IC50=3.24 μM | ||
| L1210 cells | Proliferation assay | 2 days | Antiproliferative activity against mouse L1210 cells assessed as inhibition of cell proliferation incubated for 2 days by Coulter counter based assay, IC50=8.6 μM | ||
| FM3A cells | Proliferation assay | 2 days | Antiproliferative activity against mouse FM3A cells assessed as inhibition of cell proliferation incubated for 2 days by Coulter counter based assay, IC50=3.6 μM | ||
| CEM cells | Proliferation assay | 3 days | Antiproliferative activity against human CEM cells assessed as inhibition of cell proliferation incubated for 3 days by Coulter counter based assay, IC50=3.5 μM | ||
| HeLa cells | Proliferation assay | 4 days | Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 4 days by Coulter counter based assay, IC50=1.9 μM | ||
| C6 (Rat) Glioma cell lines | Cytotoxicity assay | The compound was tested for cytotoxicity against C6 (Rat) Glioma cell lines, IC50=11 μM | |||
| CEM T-lymphocytes | Cytotoxicity assay | Cytotoxicity against CEM T-lymphocytes, IC50=2.47 μM | |||
| D283 MR (human) Glioma cell lines | Cytotoxicity assay | The compound was tested for cytotoxicity against D283 MR (human) Glioma cell lines, IC50=16.3 μM | |||
| D283 (human) Glioma cell lines | Cytotoxicity assay | The compound was tested for cytotoxicity against D283 (human) Glioma cell lines, IC50=6.8 μM | |||
| D341 (human) Glioma cell lines | Cytotoxicity assay | The compound was tested for cytotoxicity against D341 (human) Glioma cell lines, IC50=12.4 μM | |||
| Jurkat T cells | Cytotoxicity assay | Inhibitory concentration against Human Jurkat T cells, IC50=2.2 μM | |||
| MCF-7 cells | Cytotoxicity assay | In vitro cytotoxicity activity against MCF-7, IC50=0.3 μM | |||
| Molt 4/C8 cells | Cytotoxicity assay | Cytotoxicity against human Molt 4/C8 cells, IC50=3.24 μM | |||
| P388 cells | Cytotoxicity assay | Cytotoxicity evaluated against P388 cells, IC50=0.22 μM | |||
| MCF-7 | Proliferation assay | Antiproliferative activity in MCF-7 human breast cancer cells, IC50=5.7 μM | |||
| C6 glioma cell line | Cytotoxicity assay | Cytotoxicity against rat C6 glioma cell line, IC50=12.6 μM | |||
| HCT116 cells | Cytotoxicity assay | Cytotoxicity against human HCT116 cells, IC50=30.2 μM | |||
| HCT15 cells | Cytotoxicity assay | Cytotoxicity against human HCT15 cells, IC50=36.3 μM | |||
| KM12 cells | Cytotoxicity assay | Cytotoxicity against human KM12 cells, IC50=43.7 μM | |||
| SW620 cells | Cytotoxicity assay | Cytotoxicity against human SW620 cells, IC50=38.9 Μm | |||
| HCC2998 cells | Cytotoxicity assay | Cytotoxicity against human HCC2998 cells, IC50=41.7 μM | |||
| SR cells | Cytotoxicity assay | Cytotoxicity against human SR cells, IC50=1.86 μM | |||
| HSC2 cells | Cytotoxicity assay | Cytotoxicity against HSC2 cells, CC50=35 μM | |||
| HL60 cells | Cytotoxicity assay | Cytotoxicity against human HL60 cells, CC50=6 μM | |||
| HepG2 cells | Growth inhibition assay | Growth inhibition of human HepG2 cells, GI50=17 μM | |||
| INA-6 cells | Cytotoxicity assay | Cytotoxicity against human INA-6 cells assessed as viable fractions using annexin V-FITC/propidium iodide staining by flow cytometry, EC50=2 μM | |||
| PBMC cells | Cytotoxicity assay | Cytotoxicity against human PBMC cells assessed as viable fractions using annexin V-FITC/propidium iodide staining by flow cytometry, EC50=3 μM | |||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Melphalan (Alkeran, Sarcolysin, L-PAM)是氮芥的苯丙氨酸衍生物，具有抗肿瘤活性。此产品为危化品（急性毒性/易燃/皮肤腐蚀），请在穿戴防护面罩、防护手套和防护服后使用。 |
|---|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 将骨髓瘤细胞系RPMI 8226暴露于30分钟的melphalan脉冲，melphalan作为DNA交联剂，引起细胞周期进展延迟[1]。Melphalan在体外细胞中结合DNA、RNA和蛋白。Melphalan在体外人类细胞中诱导染色体畸变、姊妹染色单体互换、微核、HPRT基因的突变和DNA损伤。它还能诱导C3H 10T1/2和其他细胞的转化。除此之外，melphalan在细菌和果蝇中诱导异倍体以及伴性隐性致死突变[3]。 | |||
|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在小鼠研究中，Melphalan常以口服、腹腔注射以及皮肤给药途径进行给药。在大鼠研究中为腹腔注射，在猴子中是口服给药。在小鼠中，melphalan的处理会导致前胃乳头瘤、淋巴肉瘤、皮肤和肺肿瘤。在大鼠中，melphalan的处理会导致乳腺肿瘤和腹膜肉瘤。在猴子中melphalan的处理结果目前还不确定[3]。 | |
|---|---|---|
| 动物实验 | Animal Models | Tg.AC 小鼠 |
| Dosages | 0.25, 1和4 mg/kg/每周 | |
| Administration | 皮肤局部给药/口服 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06313502 | Not yet recruiting | Plasma Cell Disorder |
University of Arkansas|University of Iowa |
June 2024 | Phase 1 |
| NCT04455139 | Terminated | Eye Cancer Retinoblastoma |
Prof. Beck Popovic Maja|University of Lausanne Hospitals |
November 15 2021 | Phase 2 |
| NCT04945954 | Not yet recruiting | Hematopoietic Stem Cell Transplantation |
Seoul National University Hospital|National Institute of Food and Drug Safety Evaluation (Republic of Korea) |
June 2021 | Not Applicable |
|
化学信息&溶解度
| 分子量 | 305.20 | 分子式 | C13H18Cl2N2O2 |
| CAS号 | 148-82-3 | SDF | Download Melphalan SDF |
| Smiles | C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 3.5 mg/mL ( (11.46 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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