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Melphalan DNA alkylator chimico

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

N. Cat.S8266

Melphalan (Alkeran, Sarcolysin, L-PAM) è un derivato della fenilalanina della mostarda azotata con attività antineoplastica.Questo prodotto è una sostanza chimica pericolosa (tossicità acuta/infiammabile/corrosivo per la pelle). Si prega di usarlo indossando una maschera protettiva per il viso, guanti e indumenti.

Melphalan DNA alkylator chimico Chemical Structure

Struttura chimica

Peso molecolare: 305.20

Vai a

Controllo Qualità

Lotto: Purezza: 99.47%

99.47

Target correlati	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Altro DNA alkylator Inibitori	Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466) Tretazicar (CB1954) Treosulfan Semustine

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dellattività
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
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	305.20	Formula	C₁₃H₁₈Cl₂N₂O₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	148-82-3	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	Alkeran, Sarcolysin, L-PAM			Smiles	C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl

Solubilità

In vitro
Lotto:

DMSO : 3.5 mg/mL (11.46 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

In vitro	L'esposizione di una linea cellulare di mieloma (RPMI 8226) a un impulso di 30 minuti di melphalan (1-fenilalanina-mostarda) provoca un ritardo nella progressione del ciclo cellulare caratteristico degli agenti di reticolazione del DNA. È stato dimostrato che questo composto si lega a DNA, RNA e proteine nelle cellule in vitro. Induce aberrazioni cromosomiche, scambio di cromatidi fratelli, micronuclei, mutazioni nel gene HPRT e DNA Damage nelle cellule umane in vitro. Induce anche la trasformazione di cellule C3H 10T1/2 e altre cellule. Nelle cellule di roditori coltivate, induce aberrazioni cromosomiche, scambio di cromatidi fratelli, mutazioni geniche e DNA Damage. Inoltre, induce aneuploidia e mutazioni letali recessive legate al sesso in Drosophila, e mutazioni nei batteri.
In vivo	Melphalan è stato testato su topi tramite applicazione orale, intraperitoneale e dermica; su ratti tramite iniezione intraperitoneale e su scimmie tramite somministrazione orale. Nei topi, la somministrazione di questo composto ha prodotto papillomi dello stomaco anteriore, linfosarcomi e tumori della pelle e dei polmoni. Nei ratti, ha causato tumori della ghiandola mammaria e sarcomi peritoneali. I risultati sulle scimmie non sono stati conclusivi.
Riferimenti	[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/

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Supporto tecnico

Istruzioni per la manipolazione

Tel: +1-832-582-8158 Ext:3

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