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Mocetinostat (MGCD0103) HDAC 억제제

Name: Mocetinostat (MGCD0103)
Brand: Selleck Chemicals
SKU: S1122
Rating: 5 (118 reviews)

제품 번호S1122

Mocetinostat (MGCD0103, MG0103)는 세포 유리 분석에서 0.15 μM의 IC50를 가진 HDAC1에 가장 강력한 HDAC 억제제이며, HDAC2, 3 및 11에 대해 2-10배의 선택성을 가지며, HDAC4, 5, 6, 7 및 8에는 활성이 없습니다. Mocetinostat (MGCD0103)는 Apoptosis 및 Autophagy를 유도합니다. 2상.

Mocetinostat (MGCD0103) HDAC 억제제 Chemical Structure

화학 구조

분자량: 396.44

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품질 관리

배치: 순도: 99.93%

99.93

관련 타겟	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
기타 HDAC 억제제	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Tubastatin A Ricolinostat (ACY-1215) PCI-34051

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
PBMC	Apoptosis Assay	0.5/2/3 μM	24/48 h		induces apoptosis dose and time dependently	20406947
HeLa	Function Assay	10 μM	7 h	DMSO	disrupts normal spindle checkpoint function	20538840
HeLa	Function Assay	10 μM	6/12/24 h	DMSO	induces mitotic accumulation and delayed p21 expression	20538840
HeLa	Function Assay	0.3-10 μM	8 h	DMSO	increases caspase 3 and 7 activation dose dependently	20538840
HeLa	Function Assay	0.3-10 μM	8 h	DMSO	increases acetylated H3 K9 (H3K9Ac) at 10 μM	20538840
DMS114	Growth Inhibition Assay				IC50=640 nM	20682643
H82	Growth Inhibition Assay				IC50=250 nM	20682643
H146	Growth Inhibition Assay				IC50=35 nM	20682643
H526	Growth Inhibition Assay				IC50=480 nM	20682643
KM-H2	Function Assay	1 μM	0.25-48 h	DMSO	activates NF-kB	20880107
L428	Function Assay	1 μM	0.25-48 h	DMSO	activates NF-kB	20880107
HD-LM2	Function Assay	1 μM	0.25-48 h	DMSO	activates NF-kB	20880107
KM-H2	Function Assay	0.5/1 μM	24/48 h	DMSO	upregulates TNF-α dose and time dependently	20880107
L428	Function Assay	0.5/1 μM	24/48 h	DMSO	upregulates TNF-α dose and time dependently	20880107
HD-LM2	Function Assay	0.5/1 μM	24/48 h	DMSO	upregulates TNF-α dose and time dependently	20880107
KM-H2	Function Assay	1 μM	24/48 h	DMSO	downregulates XIAP, activated caspases 9 and 3	20880107
L428	Function Assay	1 μM	24/48 h	DMSO	downregulates XIAP, activated caspases 9 and 3	20880107
HD-LM2	Function Assay	1 μM	24/48 h	DMSO	downregulates XIAP, activated caspases 9 and 3	20880107
KM-H2	Apoptosis Assay	0.1/0.5/1 μM	48 h	DMSO	induces apoptosis dose dependently	20880107
L428	Apoptosis Assay	0.1/0.5/1 μM	48 h	DMSO	induces apoptosis dose dependently	20880107
HD-LM2	Apoptosis Assay	0.1/0.5/1 μM	48 h	DMSO	induces apoptosis dose dependently	20880107
KM-H2	Function Assay	0.1-2 μM	24 h	DMSO	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
L428	Function Assay	0.1-2 μM	24 h	DMSO	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
HD-LM2	Function Assay	0.1-2 μM	24 h	DMSO	shows acetylation of histone 3 and upregulation of the cell cycle regulatory protein p21	20880107
KM-H2	Growth Inhibition Assay		72 h	DMSO	IC50=2.86 μM	20880107
L428	Growth Inhibition Assay		72 h	DMSO	IC50=1.96 μM	20880107
HD-LM2	Growth Inhibition Assay		72 h	DMSO	IC50=1.88 μM	20880107
LP1	Function Assay	1 μM	24 h		enhances 5-AC-induced MAGE-A3 gene expression	21171821
ANBL6	Function Assay	1 μM	24 h		enhances 5-AC-induced MAGE-A3 gene expression	21171821
HMEC	Growth Inhibition Assay				IC50=19 μM	21317455
SW620	Growth Inhibition Assay				IC50=1 μM	21317455
SW48	Growth Inhibition Assay				IC50=0.8 μM	21317455
HT-29	Growth Inhibition Assay				IC50=0.7 μM	21317455
HCT15	Growth Inhibition Assay				IC50=0.7 μM	21317455
PAXF 1657L†	Growth Inhibition Assay				EC50=0.3 μM	21375679
PAXF 546L†	Growth Inhibition Assay				EC50=1.5 μM	21375679
Panc-1	Growth Inhibition Assay				EC50=1.8 μM	21375679
MiaPaca-2	Growth Inhibition Assay				EC50=0.6 μM	21375679
AsPC-1	Growth Inhibition Assay				EC50=3.9 μM	21375679
BxPC-3	Growth Inhibition Assay				EC50=1.1 μM	21375679
MMCs	Function Assay	1 μM	6-24 h		dose-dependently inhibits the trimethylation level of H3-K9 (H3-K9me3)	24451378
MMCs	Function Assay	1 μM	24 h		augments global acetylation levels of histone H3-K9/14 (H3-K9/14ac) and H4-K12 (H4-K12ac)	24451378
MMCs	Function Assay	1 μM	24 h		increases HAT activity	24451378
MMCs	Function Assay	0.5/1 μM	24 h		shows 45-fold stimulation in cGMP levels	24451378
MMCs	Function Assay	1 μm	0-48 h		increases NPRA protein expression 2.7–3.5 fold	24451378
Panc1	Cell Viability Assay	1 μM	72 h	DMSO	enhances gemcitabine-induces cell viability decrease	25872941
Panc1	Apoptosis Assay	1 μM	72 h	DMSO	sensitizes Panc1 cells for gemcitabine-induced apoptosis	25872941
Panc1	Function Assay	0.5/1/2.5 μM	48 h	DMSO	reduces expression of ZEB1 on both mRNA and protein level	25872941
Panc1	Function Assay	0.5/1/2.5 μM	48 h	DMSO	upregulates miR-203	25872941
MOLP8	Growth Inhibition Assay		48 h		IC50=0.6± 0.04μM	26091518
T47D	Growth Inhibition Assay		48 h		IC50=1.17 μM	26378038
MCF7	Growth Inhibition Assay		48 h		IC50=0.67 μM	26378038
BT549	Growth Inhibition Assay		48 h		IC50=4.38 μM	26378038
MDA-MB-231	Growth Inhibition Assay		48 h		IC50=3.04 μM	26378038
HEK293	Function assay				Inhibition of HDAC1 in HEK293 cells, IC50=0.13μM	18308563
HEK293	Function assay				Inhibition of HDAC3 in HEK293 cells, IC50=0.61μM	18308563
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.29μM	18570366
HCT116	Function assay				Induction of p21cip/waf1 protein expression in human HCT116 cells relative to MS275, EC50=0.45μM	18570366
Du145	Antiproliferative assay		72 hrs		Antiproliferative activity against human Du145 cells after 72 hrs by MTT assay, IC50=0.67μM	18570366
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=0.9μM	18570366
HCT116	Cell cycle assay				Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase, EC50<1μM	18570366
T24	Function assay				Induction of H3 histone acetylation in human T24 cells relative to MS275, EC50=1.38μM	18570366
HCT116	Apoptosis assay	1 uM			Induction of apoptosis in HCT116 cells at 1 uM	18570366
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells by MTT assay, IC50=0.3μM	19114304
HCT116	Function assay		16 hrs		Induction of p21WAF1/CIP1 expression in human HCT116 cells assessed as tubulin level after 16 hrs by luciferase assay, EC50=0.6μM	19114304
T24	Function assay		16 hrs		Induction of histone H4 hyperacetylation in human T24 cells after 16 hrs by immunoblotting, EC50<1μM	19114304
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50=0.31μM	21650221
H1299	Antiproliferative assay				Antiproliferative activity against human H1299 cells, IC50=1.44μM	21650221
HCT116	Antiproliferative assay				Antiproliferative activity against human HCT116 cells, IC50=0.31μM	21742496
Sf9	Function assay		2 hrs		Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50=0.102μM	23009203
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.327μM	23206867
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=1.279μM	23206867
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=4.807μM	23206867
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=0.7μM	23829483
MCF7	Cytotoxicity assay		72 hrs		Cytotoxicity against human MCF7 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=1.26μM	23829483
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=1.73μM	23829483
DU145	Cytotoxicity assay		72 hrs		Cytotoxicity against human DU145 cells assessed as growth inhibition by measuring cellular ATP level after 72 hrs by cell-titer glo assay, IC50=2.06μM	23829483
Jurkat	Apoptosis assay	1 to 10 uM	24 hrs		Induction of apoptosis in human Jurkat cells assessed as PARP cleavage at 1 to 10 uM after 24 hrs by Western blot analysis	23829483
HeLa	Function assay	1 to 10 uM	24 hrs		Inhibition of HDAC in human HeLa cells assessed as increase in H3K9Ac level at 1 to 10 uM after 24 hrs by Western blot analysis	23829483
Jurkat	Function assay	1 to 10 uM	24 hrs		Inhibition of HDAC in human Jurkat cells assessed as increase in H3K9Ac level at 1 to 10 uM after 24 hrs by Western blot analysis	23829483
High5	Function assay		3 to 24 hrs		Inhibition of human recombinant HDAC1 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay, IC50=0.95μM	24095018
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.57μM	24095018
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.65μM	24095018
High5	Function assay		3 to 24 hrs		Inhibition of human recombinant HDAC3 expressed in baculovirus infected insect high5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 to 24 hrs by fluorescence assay, IC50=1.67μM	24095018
SNU16	Cytotoxicity assay		72 hrs		Cytotoxicity against human SNU16 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.142μM	25805446
High5	Function assay		24 hrs		Inhibition of recombinant human HDAC2 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay, IC50=0.17μM	25805446
High5	Function assay		3 hrs		Inhibition of recombinant human HDAC3 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 3 hrs by fluorescence assay, IC50=0.36μM	25805446
High5	Function assay		24 hrs		Inhibition of recombinant human HDAC1 expressed in baculovirus infected insect High5 cells using Ac-Lys-Tyr-Lys (epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence assay, IC50=0.39μM	25805446
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.396μM	25805446
SW620	Cytotoxicity assay		72 hrs		Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.419μM	25805446
MKN45	Cytotoxicity assay		72 hrs		Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.61μM	25805446
Hep3B	Cytotoxicity assay		72 hrs		Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.823μM	25805446
HepG2	Cytotoxicity assay		72 hrs		Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.876μM	25805446
SNU5	Cytotoxicity assay		72 hrs		Cytotoxicity against human SNU5 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=1.009μM	25805446
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=2.08μM	25805446
SJSA1	Cytotoxicity assay		72 hrs		Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=3.624μM	25805446
MHCC97H	Cytotoxicity assay		72 hrs		Cytotoxicity against human MHCC97H cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=4.563μM	25805446
PANC1	Cytotoxicity assay		72 hrs		Cytotoxicity against human PANC1 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=26.774μM	25805446
U937	Function assay	10 uM	24 hrs		Inhibition of HDAC3 in human U937 cells assessed as increase in histone H3 lysine-9 acetylation at 10 uM incubated for 24 hrs by Western blotting method	26287310
PC3	Function assay	10 uM	24 hrs		Inhibition of HDAC3 in human PC3 cells assessed as increase in histone H3 lysine-9 acetylation at 10 uM incubated for 24 hrs by Western blotting method	26287310
U937	Function assay	10 uM	24 hrs		Inhibition of HDAC in human U937 cells assessed as reduction in cyclin E expression in at 10 uM incubated for 24 hrs by Western blotting method	26287310
Sf9	Function assay		10 mins		Inhibition of recombinant full length human C-terminal FLAG-tagged HDAC11 expressed in baculovirus infected Sf9 cells using Boc-Lys(epsilon-Ac)-AMC as substrate pretreated for 10 mins followed by substrate addition by fluorometric method, IC50=0.59μM	28501514
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Sf9	Function assay				Inhibition Assay: HDAC inhibition assays were performed by Reaction Biology Corp. (Malvern, Pa.) using isolated human, recombinant full-length HDAC1 and -6 from a baculovirus expression system in Sf9 cells, IC50=0.102μM	ChEMBL
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=1.24μM	ChEMBL
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=2.49μM	ChEMBL
HeLa	Antiproliferative assay		48 hrs		Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=3.32μM	ChEMBL
HeLa	Antiproliferative assay		72 hrs		Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=3.42μM	ChEMBL
HCT116	Antiproliferative assay		72 hrs		Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=3.51μM	ChEMBL
HepG2	Antiproliferative assay		48 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=4.05μM	ChEMBL
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=4.25μM	ChEMBL
HepG2	Antiproliferative assay		24 hrs		Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=5.79μM	ChEMBL
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=11.87μM	ChEMBL
A549	Antiproliferative assay		48 hrs		Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=14.57μM	ChEMBL
HCT116	Antiproliferative assay		24 hrs		Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=29.69μM	ChEMBL
HeLa	Antiproliferative assay		24 hrs		Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=43.8μM	ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	396.44	화학식	C₂₃H₂₀N₆O	보관 (수령일로부터)	3년-20°C분말
CAS 번호	726169-73-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	MG0103			Smiles	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4

용해도

In vitro
배치:

DMSO : 60 mg/mL (151.34 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 160 mg/mL (403.59 mM) 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 79 mg/mL (199.27 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 79 mg/mL (199.27 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 13 mg/mL (32.79 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.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.000mg/ml (5.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	8.000mg/ml (20.18mM)	Taking the 1 mL working solution as an example, add 50 μL 160 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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

Targets/IC₅₀/Ki	HDAC1 (Cell-free assay) 0.15 μM HDAC2 (Cell-free assay) 0.29 μM HDAC11 (Cell-free assay) 0.59 μM HDAC3 (Cell-free assay) 1.66 μM
시험관 내(In vitro)	Mocetinostat (MGCD0103)는 9가지 인간 재조합 HDAC 중 HDAC1, HDAC2, HDAC3, HDAC11을 포함한 일부만 나노몰 또는 낮은 마이크로몰 농도에서 용량 의존적으로 억제합니다. 시험관 내에서 인간 HDAC1 및 HDAC2 효소에 대해 가장 강력한 억제 활성을 나타내며, 클래스 II HDAC는 억제하지 않습니다. 이 화합물의 외부 고리 아미노기는 효소 억제 활성에 필요합니다. 왜냐하면 데스아미노 유사체와 함께 HDAC1 및 HDAC2에 대한 HDAC 억제 활성이 완전히 사라지기 때문입니다. 억제 활성은 6 μM에서 최대 평형에 도달하며, MGCD0103에 의해 영향을 받는 최대 억제 가능 효소 풀은 HCT116 세포에서 전체 효소 활성의 75%이며, NVP-LAQ824는 이들 세포에서 거의 100%를 억제합니다. A549 세포에서도 전체 세포에서 HDAC 활성의 용량 의존적 억제를 나타냅니다.
키나아제 분석	시험관 내 HDAC 효소 분석
키나아제 분석	탈아세틸화 효소 분석은 동질 형광 방출 분석을 기반으로 합니다. 정제된 재조합 HDAC 효소는 다양한 농도로 희석된 Mocetinostat (MGCD0103)와 함께 분석 완충액 [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl₂, 2.7 mM KCl]에서 실온에서 10분 동안 배양됩니다. 기질 Boc-Lys(ε-Ac)-AMC를 반응에 첨가하여 37 °C에서 추가로 배양합니다. 기질의 농도와 배양 시간은 HDAC 효소의 다른 아이소타입에 따라 다릅니다. 실온에서 20분간 트립신 배양하면 탈아세틸화된 기질로부터 형광 물질이 방출됩니다. 형광 신호는 360 nm 여기, 470 nm 방출 및 435 nm 컷오프에서 형광계로 감지됩니다.
생체 내(In vivo)	Mocetinostat (MGCD0103)는 누드 마우스에서 인간 종양 이종이식편의 성장을 유의하게 억제했으며, 항종양 활성은 종양 내 히스톤 아세틸화 유도와 상관관계가 있었습니다. 이 화합물(2HBr 염)의 P.O. 투여는 매일 13일 투여 후 누드 마우스에서 이식된 진행성 A549 종양의 성장을 용량 의존적으로 유의하게 감소시켰습니다. 이는 (2HBr 염 170 mg/kg, 자유 염기 120 mg/kg에 해당) 체중 변화 없이 차량 단독 치료와 비교하여 종양 성장을 유의하게 차단했습니다. 또한, 백혈구 수를 감소시키지 않으며 잘 tolerated됩니다. 이 화합물은 NSCLC H1437을 포함한 다른 많은 인간 종양 이종이식 모델에서도 경구 활성을 가집니다. 80 mg/kg (자유 염기)에서, 매일 13일 p.o. 투여 후 동물 체중 감소 없이 H1437 종양의 성장을 거의 완전히 차단합니다. 이는 폐동맥압을 더욱 극적으로 감소시킵니다. 더욱이, 이 화합물은 폐동맥 가속 시간을 개선하고 폐동맥 흐름 엔벨로프의 수축기 노칭을 감소시켜, HDAC 억제제가 폐혈관 리모델링 및 경직에 긍정적인 영향을 미친다는 것을 시사합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/18413790/ [2] https://pubmed.ncbi.nlm.nih.gov/22282194/

적용 분야

방법	바이오마커	PMID
Western blot	Ac-H3 / Ac-H4 / Ac-tubulin Bad / Bid / Bak / Puma / Bax / Cleaved caspase-9 / Cleaved caspase-3 / Cleaved PARP	29186204
Immunofluorescence	Nanog / MHC E-cadherin / ZEB1	26240433
Growth inhibition assay	Cell viability	26378038

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT04299113	Recruiting	Rhabdomyosarcoma	Jonsson Comprehensive Cancer Center\|Mirati Therapeutics Inc.\|Phase One Foundation	May 14 2020	Phase 1
NCT02993991	Withdrawn	Squamous Cell Carcinoma Head And Neck\|Squamous Cell Carcinoma Mouth\|Resectable Squamous Cell Carcinoma of Oral Cavity	University Health Network Toronto\|Mirati Therapeutics Inc.\|AstraZeneca	October 10 2017	Phase 1
NCT02236195	Completed	Urothelial Carcinoma	Mirati Therapeutics Inc.	October 2014	Phase 2
NCT00666497	Terminated	Acute Myeloid Leukemia (AML)\|Myelodysplastic Syndrome (MDS)	Mirati Therapeutics Inc.	June 2008	Phase 2
NCT00511576	Terminated	Breast Cancer\|Lung Cancer\|Pulmonary Cancer\|Non-Small-Cell Lung Carcinoma\|Prostate Cancer\|Prostatic Cancer\|Gastric Cancer\|Stomach Cancer	Mirati Therapeutics Inc.	August 2007	Phase 1

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