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Melphalan DNA alkylator chemical

Name: Melphalan
Brand: Selleck Chemicals
SKU: S8266
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S8266

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.

Chemical Structure

Molecular Weight: 305.20

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Quality Control

Batch: Purity: 99.47%

99.47

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Other DNA alkylator Inhibitors	Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466) Semustine Treosulfan Tretazicar (CB1954)

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 3.5 mg/mL (11.46 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	305.20	Formula	C₁₃H₁₈Cl₂N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	148-82-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Alkeran, Sarcolysin, L-PAM			Smiles	C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl

Mechanism of Action

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. This compound has been shown to bind to DNA, RNA, and protein in cells in vitro. It 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.
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 this compound produced forestomach papillomas, lymphosarcomas, and skin and lung tumours. In rats, it caused mammary gland tumours, and peritoneal sarcomas. Results in monkeys were inconclusive.
References	[1] https://pubmed.ncbi.nlm.nih.gov/1915798/ [2] https://pubmed.ncbi.nlm.nih.gov/11695563/ [3] https://www.ncbi.nlm.nih.gov/books/NBK304320/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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