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Decitabine DNA Methyltransferase 억제제

Name: Decitabine
Brand: Selleck Chemicals
SKU: S1200
Rating: 5 (220 reviews)

제품 번호S1200

Decitabine은 DNA methyltransferase 억제제로, DNA에 통합되어 DNA의 저메틸화와 DNA 복제의 S기 내 정지를 유발합니다. 골수이형성 증후군(MDS) 치료에 사용됩니다. Decitabine은 다양한 암세포주에서 세포 주기 정지 및 Apoptosis를 유도합니다.

Decitabine DNA Methyltransferase 억제제 Chemical Structure

화학 구조

분자량: 228.21

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품질 관리

배치: 순도: 99.90%

99.90

관련 타겟	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
기타 DNA Methyltransferase 억제제	RG108 SGI-1027 Zebularine (NSC 309132) GSK3685032 Gamma-Oryzanol CM272 β-thujaplicin Bobcat339 DC-05 2'-Deoxy-5-Fluorocytidine

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
Eca109	Function Assay	0.5 μM	24 h	water	modulates the gene expression of MAGE-A members	25123082
Eca109	Growth Inhibition Assay	0.5/2.5/5 μM	24/48/72 h	water	inhibits cell growth in both dose- and time- dependent manner	25123082
Eca109	Function Assay	0.5 μM	6/12/24 h	water	inhibits cell migration	25123082
Eca109	Function Assay	0.5 μM	24 h	water	inhibits cell invasion	25123082
Eca109	Growth Inhibition Assay	0.5 μM	24 h	water	induces G2/M arrest in the cell cycle	25123082
Eca109	Function Assay	0.5/1 μM	24 h	water	decreases expression of NF-κB2 and MMP2	25123082
SW1116	Growth Inhibition Assay	0.5/1/2/5 μM	48 h	DMSO	enhances the Gefitinib induced cell inhibition	24874286
LOVO	Growth Inhibition Assay	0.5/1/2/5 μM	48 h	DMSO	enhances the Gefitinib induced cell inhibition	24874286
SW1116	Function Assay	10 μM	48 h	DMSO	increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib	24874286
LOVO	Function Assay	10 μM	48 h	DMSO	increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib	24874286
SW1116	Apoptosis Assay	10 μM	48 h	DMSO	enhances Gefitinib-induced apoptosis	24874286
LOVO	Apoptosis Assay	10 μM	48 h	DMSO	enhances Gefitinib-induced apoptosis	24874286
RPMI-8226	Apoptosis Assay	1/2 μM	48/72/96 h	DMSO	induces cell apoptosis	24833108
OPM-2	Apoptosis Assay	1/2 μM	72/96/120 h	DMSO	induces cell apoptosis	24833108
JJN3	Apoptosis Assay	0.5/1 μM	24/48 h	DMSO	induces cell apoptosis	24833108
NCI-H929	Apoptosis Assay	1/2 μM	72/96/120 h	DMSO	induces cell apoptosis	24833108
RPMI-8226	Growth Inhibition Assay	1/2 μM	24/48/72 h	DMSO	affects cell cycle progression negatively	24833108
OPM-2	Growth Inhibition Assay	1/2 μM	24/48/72 h	DMSO	affects cell cycle progression negatively	24833108
JJN3	Growth Inhibition Assay	0.5/1 μM	24/48/72 h	DMSO	affects cell cycle progression negatively	24833108
NCI-H929	Growth Inhibition Assay	1/2 μM	24/48/72 h	DMSO	affects cell cycle progression negatively	24833108
HeLa	Kinase Assay				Ki=1000–5000 μM for hENT1	24780098
HeLa	Kinase Assay				Ki=5.6 ± 0.5 μM for hENT2	24780098
HeLa	Kinase Assay				Ki=21.6 ± 3.0 μM for hCNT1	24780098
HeLa	Kinase Assay				Ki=14.4 ± 4.6 μM for hCNT3	24780098
NB4	Function Assay	2.5/5/7.5/10 μM	24 h	DMSO	increasea the expression of precursor miR-125a	24484870
CD4+ CD25− T	Function Assay	1/5 μM			reduceS global DNA methylation	24476360
BV-173	Apoptosis Assay	0.25/0.5/0.75/1 μM	48/72/96 h	PBS	induces cell apoptosis in both dose- and time- dependent manner	24423613
ML-1	Apoptosis Assay	0.25/0.5/0.75/1 μM	48/72/96 h	PBS	induces cell apoptosis in both dose- and time- dependent manner	24423613
HL-60	Apoptosis Assay	0.25/0.5/0.75/1 μM	48/72/96 h	PBS	induces cell apoptosis in both dose- and time- dependent manner	24423613
KG-1a	Apoptosis Assay	0.25/0.5/0.75/1 μM	48/72/96 h	PBS	induces cell apoptosis in both dose- and time- dependent manner	24423613
BV-173	Function Assay	250/500nM	48 h	PBS	induces delayed and sustained ROS increase	24423613
CEM	Function Assay	250/500nM	48 h	PBS	induces delayed and sustained ROS increase	24423613
HL-60	Function Assay	250/500nM	48 h	PBS	induces delayed and sustained ROS increase	24423613
ML-1	Function Assay	250/500nM	48 h	PBS	induces delayed and sustained ROS increase	24423613
DLD-1	Function Assay	250/500nM	48 h	PBS	do not induces delayed and sustained ROS increase	24423613
HCT-116	Function Assay	250/500nM	48 h	PBS	do not induces delayed and sustained ROS increase	24423613
U937-A/E-9/14/18	Apoptosis Assay	0.01/0.1/1/10 μM	48 h		induces cell apoptosis in a dose-dependent manner	24300456
HT29	Growth Inhibition Assay		72 h		IC50=1400±179 μM	24172061
SW48	Growth Inhibition Assay		72 h		IC50=15.2±6.2 μM	24172061
HCT116	Growth Inhibition Assay		72 h		IC50=1.7±0.4 μM	24172061
HepG2	Function Assay	0.5/1 μM	24 h	DMSO	up-regulated the relative OCTN2 mRNA and protein expression	24146874
LS174T	Function Assay	0.5/1 μM	24 h	DMSO	lead to an increase of OCTN2 levels	24146874
HepG2	Apoptosis Assay	1/10/100 μM	7 d	DMSO	induces cell apoptosis in a dose-dependent manner	24146874
LS174T	Apoptosis Assay	1/10/100 μM	7 d	DMSO	induces cell apoptosis in a dose-dependent manner	24146874
QBC-939	Apoptosis Assay	1/10/100 μM	7 d	DMSO	induces cell apoptosis in a dose-dependent manner	24146874
U251	Apoptosis Assay	1/10/100 μM	7 d	DMSO	induces cell apoptosis in a dose-dependent manner	24146874
HL-60	Growth Inhibition Assay	1 μM	48 h		increases G2-phase cell fraction	24000324
MDA‑MB‑453	Function Assay	0.2/1 μM	72 h		causes re-expression of claudin 1	23844228
HCC1569	Function Assay	0.2/1 μM	72 h		causes re-expression of claudin 1	23844228
BT‑474	Function Assay	0.2/1 μM	72 h		causes re-expression of claudin 1	23844228
AGS	Apoptosis Assay	5/10/20/50 μM	48 h	DMSO	inhibits the cell viability	23582784
A549	Apoptosis Assay	5/10/20/50 μM	48 h	DMSO	inhibits the cell viability	23582784
AGS	Growth Inhibition Assay	5/10/20/50 μM	48 h	DMSO	induces G2/M phase arrest	23582784
Kasumi-1	Apoptosis Assay	0.5 μM	48 h		decreases the cell viability co-treated with Tf-NP-sc	23493348
OCI-AML3	Apoptosis Assay	2.5 μM	48 h		decreases the cell viability co-treated with Tf-NP-sc	23493348
MV4-11	Apoptosis Assay	2.5 μM	48 h		decreases the cell viability co-treated with Tf-NP-sc	23493348
NK	Cytotoxity Assay	0.02-20 μM	5 d		decreases the cytolytic activity of NK cells at intermediate concentrations resulting in a U-shaped dose–response curve	23328088
NK	Apoptosis Assay	0.02-20 μM	5 d		decrease NK cell proliferation and viability as the concentration increased	23328088
NK	Function Assay	0.01-20 μM	5 d		causes hypomethylation of NK cells in a dose–response	23328088
MOLT4/DNR	Function Assay	5 μM	4 d		reduces ABCB1 mRNA expression	23060570
Jurkat/DOX	Function Assay	5 μM	4 d		reduces ABCB1 mRNA expression	23060570
MOLT4/DNR	Growth Inhibition Assay	5 μM	4 d		reduces the IC50 value for daunorubicin sensitivity	23060570
Jurkat/DOX	Growth Inhibition Assay	5 μM	4 d		reduces the IC50 value for daunorubicin sensitivity	23060570
ccRCC	Apoptosis Assay	0.01-10μM	72 h	DMSO	has minimal effect on cell proliferation	22826467
TNBC	Apoptosis Assay	0.01-10μM	72 h	DMSO	has minimal effect on cell proliferation	22826467
A498	Apoptosis Assay	0.01-10μM	72 h	DMSO	induces synergistic responses with romidepsin	22826467
KIJ265T	Apoptosis Assay	0.01-10μM	72 h	DMSO	induces synergistic responses with romidepsin	22826467
MDA-231	Apoptosis Assay	0.01-10μM	72 h	DMSO	induces synergistic responses with romidepsin	22826467
BT-20	Apoptosis Assay	0.01-10μM	72 h	DMSO	induces synergistic responses with romidepsin	22826467
U937	Growth Inhibition Assay	5-20 μM	24/48/72 h		induces a decrease in cell viability in a concentration- and time-dependent manner	22767021
HL60	Growth Inhibition Assay	5-20 μM	24/48/72 h		induces a decrease in cell viability in a concentration- and time-dependent manner	22767021
U937	Apoptosis Assay	15 μM	24/48/72 h		induces cell apoptosis	22767021
HL60	Apoptosis Assay	15 μM	24/48/72 h		induces cell apoptosis	22767021
LS411N	Apoptosis Assay	0.5 μM	72 h		increases Fas mRNA level	22461695
MDA-MB-231	Apoptosis Assay	10 μM	48 h		reduces cell viability in a dose-dependent manner	21887697
MCF-7	Apoptosis Assay	10 μM	48 h		reduces cell viability in a dose-dependent manner	21887697
A375	Growth Inhibition Assay	0.5 μM	1/5/8 d		inhibits proliferation and induces differentiation of melanoma cells	21796622
SKMEL1	Growth Inhibition Assay	0.5 μM	1/5/8 d		inhibits proliferation and induces differentiation of melanoma cells	21796622
SKMEL3	Growth Inhibition Assay	0.5 μM	1/5/8 d		inhibits proliferation and induces differentiation of melanoma cells	21796622
SKMEL28	Growth Inhibition Assay	0.5 μM	1/5/8 d		inhibits proliferation and induces differentiation of melanoma cells	21796622
MeWo	Growth Inhibition Assay	0.5 μM	1/5/8 d		inhibits proliferation and induces differentiation of melanoma cells	21796622
B16	Growth Inhibition Assay	0.5 μM	1/5/8 d		inhibits proliferation and induces differentiation of melanoma cells	21796622
Ly 1	Growth Inhibition Assay		24 h		IC50=7.3 μM	21772049
Ly 7	Growth Inhibition Assay		24 h		IC50=10.7 μM	21772049
Su-DHL6	Growth Inhibition Assay		24 h		IC50＞20 μM	21772049
Ly 10	Growth Inhibition Assay		24 h		IC50＞20 μM	21772049
RIVA	Growth Inhibition Assay		24 h		IC50＞20 μM	21772049
Su-DHL2	Growth Inhibition Assay		24 h		IC50＞20 μM	21772049
Ly 1	Growth Inhibition Assay		48 h		IC50=0.34 μM	21772049
Ly 7	Growth Inhibition Assay		48 h		IC50=0.025 μM	21772049
Su-DHL6	Growth Inhibition Assay		48 h		IC50＞20 μM	21772049
Ly 10	Growth Inhibition Assay		48 h		IC50=1.8 μM	21772049
RIVA	Growth Inhibition Assay		48 h		IC50＞20 μM	21772049
Su-DHL2	Growth Inhibition Assay		48 h		IC50=17.4 μM	21772049
Ly 1	Growth Inhibition Assay		72 h		IC50=0.01 μM	21772049
Ly 7	Growth Inhibition Assay		72 h		IC50=0.018 μM	21772049
Su-DHL6	Growth Inhibition Assay		72 h		IC50=1.6 μM	21772049
Ly 10	Growth Inhibition Assay		72 h		IC50=1.2 μM	21772049
RIVA	Growth Inhibition Assay		72 h		IC50＞20 μM	21772049
Su-DHL2	Growth Inhibition Assay		72 h		IC50=11.2 μM	21772049
U373-MAGI	Antiviral assay	0.25 to 8 uM	2 to 72 hrs		Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in U5-gag level at 0.25 to 8 uM after 2 to 72 hrs by qPCR method	27117260
U373-MAGI	Antiviral assay	0.25 to 8 uM	2 to 72 hrs		Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in gag level at 0.25 to 8 uM after 2 to 72 hrs by qPCR method	27117260
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	228.21	화학식	C₈H₁₂N₄O₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	2353-33-5	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716			Smiles	C1C(C(OC1N2C=NC(=NC2=O)N)CO)O

용해도

In vitro
배치:

DMSO : 45 mg/mL (197.18 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 22.5 mg/mL

Ethanol : Insoluble

DMSO : 45 mg/mL (197.18 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 45 mg/mL

Ethanol : Insoluble

DMSO : 46 mg/mL (201.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 15 mg/mL

Ethanol : Insoluble

DMSO : 46 mg/mL (201.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 20 mg/mL

Ethanol : Insoluble

DMSO : 46 mg/mL (201.56 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 46 mg/mL

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.
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.
Clear solution	water Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	10.000mg/ml (43.82mM)	Taking the 1 mL working solution as an example, add 10 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

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

Targets/IC₅₀/Ki	DNA methylation (HL-60, KG1a cells)
시험관 내(In vitro)	Decitabine은 HL-60 및 KG1a 백혈병 세포에서 72시간 및 96시간 노출 시 각각 약 438 nM 및 43.8 nM의 IC50로 용량 및 시간 의존적으로 세포 성장을 억제합니다. 최근 연구에 따르면 이 화합물은 역형성 대세포 림프종(ALCL)에 대해 높은 항증식 및 Apoptosis 유도 활성을 보이며, KARPAS-299 세포에서 [³H]–티미딘 섭취를 0.49 μM의 EC50으로 억제합니다.
키나아제 분석	DNA 합성 분석
키나아제 분석	DNA 합성 속도는 방사성 티미딘의 DNA 통합을 통해 측정됩니다. HL-60 및 KG1a 세포는 10% 태아 혈청을 포함하는 2 mL RPMI 배지에 6웰(직경 35 mm) 접시에 현탁되어 해당 약물들의 다양한 농도로 48시간 동안 배양됩니다(약물은 동시에 첨가됨). 48시간 후, 0.5 μCi [³H] 티미딘(6.7 Ci/mmol)이 각 웰에 첨가되고 추가로 24시간 동안 배양됩니다. 세포는 GF/C 유리 섬유 필터(직경 2.4 cm)에 놓고 차가운 0.9% NaCl, 5% 차가운 트리클로로아세트산 및 에탄올로 세척합니다. DNA를 포함하는 필터는 건조시킨 다음 EcoLite 신틸레이션 액(ICN)에 넣고 Beckman LS 6000IC 신틸레이션 카운터를 사용하여 방사능을 측정합니다. IC50은 용량-반응 곡선에서 백혈병 세포주의 DNA 합성을 50% 억제하는 약물 농도로 정의됩니다.
생체 내(In vivo)	ALK+ KARPAS-299 마우스 이종이식 모델에서 2.5 mg/kg 용량의 Decitabine은 종양 세포의 Apoptosis 증가 및 증식 감소를 유발하며, 또한 종양 억제제 p16INK4A의 탈메틸화를 초래합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/12620295/ [2] https://pubmed.ncbi.nlm.nih.gov/22687603/

적용 분야

방법	바이오마커	PMID
Western blot	Survivin / Bcl-2 / p53 / c-Myc / DNMT1 p-AKT / AKT / p-GSK3β / GSK3β / p-Myc / Myc / p-P70 / P70 / p-4EBP-1 / 4EBP-1 / PTEN phospho-p38 / p38 / phospho-NFκB / NFκB p-JAK1 / JAK1 / p-JAK2 / JAK2 / p-STAT3 / STAT3 E-cadherin / N-cadherin / Snail / MMP-2 / MMP-9 / Bcl-2 / Bax	26384351
Immunofluorescence	DNMT1 E-cadherin / MMP-9	21303982
Growth inhibition assay	Cell viability	26384351

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT06291285	Not yet recruiting	Healthy Volunteers	Novo Nordisk A/S	February 27 2024	Phase 1
NCT05960773	Recruiting	Mesothelioma\|Malignant Mesothelioma (MM)\|Early-stage Mesothelioma\|Subclinical Mesothelioma\|BRCA1-Associated Protein-1 (BAP1) Mutations\|Early-stage BAP1-associated Malignancies	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	January 31 2024	Phase 2
NCT05835011	Terminated	Myelodysplastic Syndromes	Astex Pharmaceuticals Inc.	July 14 2023	Phase 2
NCT05816356	Recruiting	Healthy	EpiDestiny Inc.\|Worldwide Clinical Trials	March 24 2023	Phase 1

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자주 묻는 질문

질문 1:
Is it a racemic mixture or a monomer?

답변:
Its S1200 is R form.

C1=C0/X	C1:	LOG(C1):
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):
C8=C7/X	C8:	LOG(C8):