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Melphalan

别名: Alkeran, Sarcolysin, L-PAM 中文名称：米尔法兰

目录号：S8266

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

规格	价格	库存
100mg	795.41	现货
500mg	3252	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

Melphalan相关产品

相关靶点	AGT	点击展开
相关产品	Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466)	点击展开
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	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	12781188
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	2590277
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	7996544
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	17416532
RT4 cells	Cytotoxicity assay	96 h	Cytotoxicity against human RT4 cells after 96 hrs by microtiter assay, IC50=14.25 μM	18187237
RT112 cells	Cytotoxicity assay	96 h	Cytotoxicity against human RT112 cells after 96 hrs by microtiter assay, IC50=4.69 μM	18187237
5637 cells	Cytotoxicity assay	96 h	Cytotoxicity against human 5637 cells after 96 hrs by microtiter assay, IC50=0.31 μM	18187237
KYSE70 cells	Cytotoxicity assay	96 h	Cytotoxicity against human KYSE70 cells after 96 hrs by microtiter assay, IC50=16.16 μM	18187237
KYSE510	Cytotoxicity assay	96 h	Cytotoxicity against human KYSE510 cells after 96 hrs by microtiter assay, IC50=8.18 Μm	18187237
KYSE520 cells	Cytotoxicity assay	96 h	Cytotoxicity against human KYSE520 cells after 96 hrs by microtiter assay, IC50=10.49 μM	18187237
YAPC cells	Cytotoxicity assay	96 h	Cytotoxicity against human YAPC cells after 96 hrs by microtiter assay, IC50=5.95 μM	18187237
DAN-G cells	Cytotoxicity assay	96 h	Cytotoxicity against human DAN-G cells after 96 hrs by microtiter assay, IC50=2.65 μM	18187237
SISO cells	Cytotoxicity assay	96 h	Cytotoxicity against human SISO cells after 96 hrs by microtiter assay, IC50=1 μM	18187237
LCLC-103H cells	Cytotoxicity assay	96 h	Cytotoxicity against human LCLC-103H cells after 96 hrs by microtiter assay, IC50=4 μM	18187237
MCF7 cells	Cytotoxicity assay	96 h	Cytotoxicity against human MCF7 cells after 96 hrs by microtiter assay, IC50=3.71 μM	18187237
A427 cells	Cytotoxicity assay	96 h	Cytotoxicity against human A427 cells after 96 hrs by microtiter assay, IC50=5.13 μM	18187237
Caov3 cells	Cytotoxicity assay	72 h	Cytotoxicity against human Caov3 cells after 72 hrs by MTT assay	19046794
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	21122952
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	21122952
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	21146985
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	21146985
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	21146985
SH-SY5Y cells	Cytotoxicity assay	72 h	Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay, IC50=5.5 μM	22633834
U251 cells	Cytotoxicity assay	5 days	Cytotoxicity against human U251 cells after 5 days by MTT assay, IC50=3 μM	24900418
A549 cells	Cytotoxicity assay	5 days	Cytotoxicity against human A549 cells after 5 days by MTT assay, IC50=3 μM	24900418
PANC1 cells	Cytotoxicity assay	5 days	Cytotoxicity against human PANC1 cells after 5 days by MTT assay, IC50=3 μM	24900418
HT-29 cells	Cytotoxicity assay	5 days	Cytotoxicity against human HT-29 cells after 5 days by MTT assay, IC50=3 μM	24900418
DLD1 cells	Cytotoxicity assay	5 days	Cytotoxicity against human DLD1 cells after 5 days by MTT assay, IC50=3 μM	24900418
HeLa cells	Cytotoxicity assay	4 days	Cytotoxicity against human HeLa cells after 4 days by Coulter counter analysis, IC50=1.9 μM	23537942
FM3A cells	Cytotoxicity assay	2 days	Cytotoxicity against mouse FM3A cells after 2 days by Coulter counter analysis, IC50=3.6 μM	23537942
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	23537942
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	24657568
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	26141911
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	26141911
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	26141911
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	26141911
C6 (Rat) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against C6 (Rat) Glioma cell lines, IC50=11 μM	9171882
CEM T-lymphocytes	Cytotoxicity assay		Cytotoxicity against CEM T-lymphocytes, IC50=2.47 μM	11170648
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	9171882
D283 (human) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against D283 (human) Glioma cell lines, IC50=6.8 μM	9171882
D341 (human) Glioma cell lines	Cytotoxicity assay		The compound was tested for cytotoxicity against D341 (human) Glioma cell lines, IC50=12.4 μM	9171882
Jurkat T cells	Cytotoxicity assay		Inhibitory concentration against Human Jurkat T cells, IC50=2.2 μM	8464041
MCF-7 cells	Cytotoxicity assay		In vitro cytotoxicity activity against MCF-7, IC50=0.3 μM	11985479
Molt 4/C8 cells	Cytotoxicity assay		Cytotoxicity against human Molt 4/C8 cells, IC50=3.24 μM	11170648
P388 cells	Cytotoxicity assay		Cytotoxicity evaluated against P388 cells, IC50=0.22 μM	9767639
MCF-7	Proliferation assay		Antiproliferative activity in MCF-7 human breast cancer cells, IC50=5.7 μM	15658875
C6 glioma cell line	Cytotoxicity assay		Cytotoxicity against rat C6 glioma cell line, IC50=12.6 μM	16970409
HCT116 cells	Cytotoxicity assay		Cytotoxicity against human HCT116 cells, IC50=30.2 μM	16996657
HCT15 cells	Cytotoxicity assay		Cytotoxicity against human HCT15 cells, IC50=36.3 μM	16996657
KM12 cells	Cytotoxicity assay		Cytotoxicity against human KM12 cells, IC50=43.7 μM	16996657
SW620 cells	Cytotoxicity assay		Cytotoxicity against human SW620 cells, IC50=38.9 Μm	16996657
HCC2998 cells	Cytotoxicity assay		Cytotoxicity against human HCC2998 cells, IC50=41.7 μM	16996657
SR cells	Cytotoxicity assay		Cytotoxicity against human SR cells, IC50=1.86 μM	16996657
HSC2 cells	Cytotoxicity assay		Cytotoxicity against HSC2 cells, CC50=35 μM	17383883
HL60 cells	Cytotoxicity assay		Cytotoxicity against human HL60 cells, CC50=6 μM	17383883
HepG2 cells	Growth inhibition assay		Growth inhibition of human HepG2 cells, GI50=17 μM	18068362
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	22019229
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	22019229
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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
https://www.ncbi.nlm.nih.gov/pubmed/1915798 https://www.ncbi.nlm.nih.gov/pubmed/11695563 https://www.ncbi.nlm.nih.gov/books/NBK304320/

参考文献

https://www.ncbi.nlm.nih.gov/pubmed/1915798
https://www.ncbi.nlm.nih.gov/pubmed/11695563
https://www.ncbi.nlm.nih.gov/books/NBK304320/

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体内溶解配方
批次：

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

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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操作手册

如果有其他问题，请给我们留言。

* 必填项

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C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
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