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Melphalan DNA alkylator 화학물

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

제품 번호S8266

Melphalan (Alkeran, Sarcolysin, L-PAM)은 질소 머스타드의 페닐알라닌 유도체로 항종양 활성을 가지고 있습니다.이 제품은 유해 화학물질(급성 독성/인화성/피부 부식성)입니다. 보호 안면 마스크, 장갑, 보호복을 착용하고 사용하십시오.

Melphalan DNA alkylator 화학물 Chemical Structure

화학 구조

분자량: 305.20

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품질 관리

배치: 순도: 99.47%

99.47

관련 타겟	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
기타 DNA alkylator 억제제	Lomeguatrib Methyl methanesulfonate Lobaplatin (D-19466) Tretazicar (CB1954) Treosulfan Semustine

세포 배양, 처리 및 작업 농도

세포주	분석 유형	배양 시간	활성 설명
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	305.20	화학식	C₁₃H₁₈Cl₂N₂O₂	보관 (수령일로부터)	3년-20°C분말
CAS 번호	148-82-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Alkeran, Sarcolysin, L-PAM			Smiles	C1=CC(=CC=C1CC(C(=O)O)N)N(CCCl)CCCl

용해도

In vitro
배치:

DMSO : 3.5 mg/mL (11.46 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 3.5 mg/mL (11.46 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 10 mg/mL (32.76 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
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.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

시험관 내(In vitro)	골수종 세포주(RPMI 8226)를 30분간 Melphalan (1-phenylalanine-mustard) 펄스에 노출시키면 DNA cross-linking agents의 특징적인 세포 주기 진행 지연이 발생합니다. 이 화합물은 시험관 내 세포에서 DNA, RNA 및 단백질에 결합하는 것으로 나타났습니다. 이는 시험관 내 인간 세포에서 염색체 이상, 자매 염색분체 교환, 미세핵, HPRT 유전자 돌연변이 및 DNA Damage를 유발합니다. 또한 C3H 10T1/2 및 기타 세포의 변형을 유발합니다. 배양된 설치류 세포에서 염색체 이상, 자매 염색분체 교환, 유전자 돌연변이 및 DNA Damage를 유발합니다. 또한, 초파리에서 이수성 및 성염색체 연관 열성 치사 돌연변이를 유발하며, 박테리아에서 돌연변이를 유발합니다.
생체 내(In vivo)	Melphalan은 경구, 복강내 및 피부 적용을 통해 생쥐에서, 복강내 주사를 통해 쥐에서, 경구 투여를 통해 원숭이에서 테스트되었습니다. 생쥐에서 이 화합물의 투여는 전위 유두종, 림프육종, 피부 및 폐 종양을 유발했습니다. 쥐에서는 유선 종양 및 복막 육종을 유발했습니다. 원숭이에서의 결과는 결정적이지 않았습니다.
참조	[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/

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
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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