Melphalan

Synonyms: Alkeran, Sarcolysin, L-PAM

Melphalan (Alkeran, Sarcolysin, L-PAM) is a phenylalanine derivative of nitrogen mustard with antineoplastic activity.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.

Melphalan Chemical Structure

Melphalan Chemical Structure

CAS No. 148-82-3

Purity & Quality Control

Melphalan Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
K562 Cytotoxicity assay 1 h In vitro cytotoxic activity against human leukemic cell line K562 after incubation for 1 hour, IC50=30 μM 12781188
Jurkat T cells Cytotoxicity assay Inhibitory concentration against Human Jurkat T cells, IC50=2.2 μM 8464041
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
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
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
HepG2 cells Growth inhibition assay Growth inhibition of human HepG2 cells, GI50=17 μM 18068362
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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description Melphalan (Alkeran, Sarcolysin, L-PAM) is a phenylalanine derivative of nitrogen mustard with antineoplastic activity.This product is a hazardous chemical (acute toxicity/flammable/skin corrosive). Please use it while wearing a protective face mask, gloves, and clothing.
In vitro
In vitro Exposure of a myeloma cell line (RPMI 8226) to a 30-minute pulse of melphalan (1-phenylalanine-mustard) results in a cell cycle progression delay characteristic for DNA cross-linking agents[1]. Melphalan has been shown to bind to DNA, RNA, and protein in cells in vitro. Melphalan induces chromosomal aberrations, sister chromatid exchange, micronuclei, mutations at the HPRT gene, and DNA damage in human cells in vitro. It also induces transformation of C3H 10T1/2 and other cells. In cultured rodent cells, it induces chromosomal aberrations, sister chromatid exchange, gene mutations, and DNA damage. In addition, it induces aneuploidy and sex-linked recessive lethal mutations in Drosophila, and mutation in bacteria[3].
In Vivo
In vivo Melphalan has been tested in mice by oral, intraperitoneal, and dermal application; in rats by intraperitoneal injection, and in monkeys by oral administration. In mice, the administration of melphalan produced forestomach papillomas, lymphosarcomas, and skin and lung tumours. In rats, melphalan caused mammary gland tumours, and peritoneal sarcomas. Results in monkeys were inconclusive[3].
Animal Research Animal Models Tg.AC mice
Dosages 0.25, 1, and 4 mg/kg weekly
Administration Topical administration/oral gavage
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

Chemical Information & Solubility

Molecular Weight 305.20 Formula

C13H18Cl2N2O2

CAS No. 148-82-3 SDF Download Melphalan SDF
Smiles C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 3.5 mg/mL ( (11.46 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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