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Ricolinostat (ACY-1215) HDAC 억제제

Name: Ricolinostat (ACY-1215)
Brand: Selleck Chemicals
SKU: S8001
Rating: 5 (71 reviews)

제품 번호S8001

Ricolinostat (ACY-1215, Rocilinostat)는 무세포 분석에서 IC50 5nM의 선택적 HDAC6 억제제입니다. HDAC1/2/3 (클래스 I HDAC)보다 HDAC6에 대해 >10배 더 선택적이며, HDAC8에 대해 약한 활성을 보이고, HDAC4/5/7/9/11, Sirtuin1, Sirtuin2에 대해 최소한의 활성을 보입니다. Ricolinostat (ACY-1215)는 세포 증식을 억제하고 apoptosis를 촉진합니다. 2상.

Ricolinostat (ACY-1215) HDAC 억제제 Chemical Structure

화학 구조

분자량: 433.5

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품질 관리

배치: 순도: 99.96%

99.96

함께 자주 사용되는 제품 Ricolinostat (ACY-1215)

(+)-JQ1

It and JQ1 increase apoptosis, diminish the expression of c-MYC and BCL-2, and lower multiple myeloma cells proliferation.

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 Mocetinostat (MGCD0103) PCI-34051

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
A-172	Growth Inhibition Assay	10 nM	24/48 h	inhibits cell growth time dependently	26150340
U87MG	Growth Inhibition Assay	10 nM	24/48 h	inhibits cell growth time dependently	26150340
Hbl-1	Growth Inhibition Assay		48 h	IC50=1.6 μM	26116270
OCI-Ly10	Growth Inhibition Assay		48 h	IC50=0.9 μM	26116270
Riva	Growth Inhibition Assay		48 h	IC50=2.2 μM	26116270
Su-DHL2	Growth Inhibition Assay		48 h	IC50=3.3 μM	26116270
OCI-Ly1	Growth Inhibition Assay		48 h	IC50=2.4 μM	26116270
OCI-Ly7	Growth Inhibition Assay		48 h	IC50=1.2 μM	26116270
Su-DHL4	Growth Inhibition Assay		48 h	IC50=4.7 μM	26116270
Su-DHL6	Growth Inhibition Assay		48 h	IC50=3.2 μM	26116270
Hbl-2	Growth Inhibition Assay		48 h	IC50=1.9 μM	26116270
Jeko-1	Growth Inhibition Assay		48 h	IC50=1.5 μM	26116270
Jvm-2	Growth Inhibition Assay		48 h	IC50=4.0 μM	26116270
Rec-1	Growth Inhibition Assay		48 h	IC50=2.3 μM	26116270
CCL-119	Growth Inhibition Assay		48 h	IC50=1.7 μM	26116270
H9	Growth Inhibition Assay		48 h	IC50=1.2 μM	26116270
HH	Growth Inhibition Assay		48 h	IC50=2.5 μM	26116270
Sup-T1	Growth Inhibition Assay		48 h	IC50=1.6 μM	26116270
MM.1S	Function Assay	0-5μM	6 h	increases acetylated α-tubulin	22262760
MM.1S	Function Assay	0.25/1μM	18 h	increases acetylated α-tubulin	22262760
MM.1R	Function Assay	0.25/1μM	18 h	increases acetylated α-tubulin	22262760
RPMI8226	Function Assay	0.25/1μM	18 h	increases acetylated α-tubulin	22262760
MM.1S	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
OPM1	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
RPMI	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
MM.1R	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
LR5	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
OPM2	Cell Viability Assay	0-8μM	48 h	decreases MM-cell viability in a dose-dependent manner	22262760
Sf9	Function assay		10 mins	Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.0047 μM.	28038324
Sf9	Function assay		15 mins	Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.009 μM.	29500130
Sf9	Function assay		15 mins	Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate additi, IC50 = 0.037 μM.	29500130
Sf9	Function assay		10 mins	Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.048 μM.	28038324
Sf9	Function assay		10 mins	Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.058 μM.	28038324
Sf9	Function assay		15 mins	Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.066 μM.	29500130
Sf9	Function assay		15 mins	Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass, IC50 = 0.1 μM.	29500130
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 1 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.29 μM.	30365892
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 4 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.54 μM.	30365892
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 2 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.58 μM.	30365892
RPMI8226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay, IC50 = 1.468 μM.	26443078
SEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.61 μM.	30365892
SUP-B15	Cytotoxicity assay		72 hrs	Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.92 μM.	30365892
RPMI18226	Cytotoxicity assay		72 hrs	Cytotoxicity against human RPMI18226 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.97 μM.	30365892
HL60	Cytotoxicity assay		72 hrs	Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 2.36 μM.	30365892
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM.	29940115
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM.	29940115
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM.	29940115
KCL22	Cytotoxicity assay		72 hrs	Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.38 μM.	30365892
U266	Cytotoxicity assay		72 hrs	Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.52 μM.	30365892
SUP-B15	Cytotoxicity assay		72 hrs	Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.54 μM.	30365892
KCL22	Cytotoxicity assay		72 hrs	Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.75 μM.	30365892
HL60	Antiproliferative assay		48 hrs	Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM.	29940115
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM.	29940115
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM.	29940115
BCP-ALL	Cytotoxicity assay		72 hrs	Cytotoxicity against human BCP-ALL cells derived from patient 3 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 4.45 μM.	30365892
MV4-11	Function assay	1000 nM	6 hrs	Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 1000 nM after 6 hrs by Western blot analysis	26443078
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
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
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
HL60	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
HL60	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
HL60	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human HL60 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in human SEM cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SUP-B15	Function assay	0.1 to 10 uM	24 hrs	Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay	30365892
SEM	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human SEM cells at IC50 to 2 times IC50 after 24 to 72 hrs by trypan exclusion method	30365892
HEL	Cell cycle assay	1 to 10 uM	48 hrs	Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 10 uM after 48 hrs propidium iodide staining based flow cytometry	29940115
SEM	Function assay		18 hrs	Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at IC50 after 18 hrs by fluorescence microscopic method	30365892
SEM	Function assay	1.6 uM	18 hrs	Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at 1.6 uM after 18 hrs by FACS analysis	30365892
SH-SY5Y	Function assay	0.1 to 1 uM	24 hrs	Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylation of alpha-tubulin at 0.1 to 1 uM after 24 hrs by Western blot analysis	30028616
SH-SY5Y	Function assay	0.1 to 1 uM	24 hrs	Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as increase in acetylation of histone H3 at 0.1 to 1 uM after 24 hrs by Western blot analysis	30028616
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	433.5	화학식	C₂₄H₂₇N₅O₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1316214-52-4	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	Rocilinostat			Smiles	C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

용해도

In vitro
배치:

DMSO : 42 mg/mL (96.88 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 86 mg/mL (198.38 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 217 mg/mL (500.57 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 87 mg/mL (200.69 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 87 mg/mL (200.69 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.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.000mg/ml (9.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 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.
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 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	5.000mg/ml (11.53mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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.
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.	4.000mg/ml (9.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of 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.

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

특징	Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA.
Targets/IC₅₀/Ki	HDAC6 (Cell-free assay) 4.7 nM HDAC2 (Cell-free assay) 48 nM HDAC3 (Cell-free assay) 51 nM HDAC1 (Cell-free assay) 58 nM HDAC8 (Cell-free assay) 100 nM
시험관 내(In vitro)	ACY-1215는 히드록삼산 유도체입니다. ACY-1215는 각각 HDAC1, HDAC2, HDAC3(클래스 I HDAC)에 대해 12배, 10배, 11배 덜 활성입니다. ACY-1215는 HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1 및 Sirtuin2에 대해 최소한의 활성(IC50 > 1μM)을 가지며, HDAC8에 대해 약간의 활성(IC50 = 0.1μM)을 가집니다. T세포 독성에 대한 ACY-1215의 IC50 값은 2.5μM입니다. ACY-1215는 BMSC 및 BM 미세환경의 사이토카인에 의해 부여되는 종양 세포 성장 및 생존을 극복합니다.
키나아제 분석	HDAC 효소 분석
키나아제 분석	ACY-1215는 분석 완충액 [50mM HEPES, pH 7.4, 100mM KCl, 0.001% Tween-20, 0.05% BSA, 20μM tris(2-carboxyethyl)phosphine]에 용해된 후 최종 농도의 6배로 희석됩니다. HDAC 효소는 분석 완충액에 최종 농도의 1.5배로 희석되어 기질 첨가 전 ACY-1215와 10분 동안 전배양됩니다. 각 효소에 사용되는 FTS(HDAC1, HDAC2, HDAC3, HDAC6) 또는 MAZ-1675(HDAC4, HDAC5, HDAC7, HDAC8, HDAC9)의 양은 적정 곡선에 의해 결정된 Michaelis 상수(Km)와 같습니다. FTS 또는 MAZ-1675는 분석 완충액에 서열 분석 등급 트립신 0.3μM과 함께 최종 농도의 6배로 희석됩니다. 기질/트립신 혼합물이 효소/화합물 혼합물에 첨가되고 플레이트는 60초 동안 흔들린 후 SpectraMax M5 마이크로플레이트 리더에 놓입니다. 효소 반응은 펩타이드 기질의 리신 측쇄 탈아세틸화 후 30분 동안 7-아미노-4-메톡시-쿠마린 방출을 모니터링하며, 반응의 선형 속도가 계산됩니다.
생체 내(In vivo)	ACY-1215는 종양 조직에 쉽게 흡수됩니다. 또한, 투여 후 24시간 이내에 혈액 세포와 종양 조직에서 아세틸화된 α-튜불린의 평행한 감소로 입증되듯이, 이 약물은 종양 조직에 축적되지 않습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/22262760/

적용 분야

방법	바이오마커	PMID
Western blot	Ac-α-tubulin / Ac-Histone H4 Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1 Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK Ac-β-catenin(K49) / p-β-catenin / β-catenin	31015208
Immunofluorescence	β-tubulin / β-catenin	25546293
Growth inhibition assay	Cell viability	31015208

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT02632071	Completed	Metastatic Breast Cancer\|Breast Carcinoma	Columbia University\|Acetylon Pharmaceuticals Incorporated\|National Cancer Institute (NCI)	March 1 2016	Phase 1
NCT01583283	Completed	Multiple Myeloma	Celgene	July 12 2012	Phase 1
NCT01323751	Completed	Multiple Myeloma	Celgene\|The Leukemia and Lymphoma Society	July 2011	Phase 1\|Phase 2

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질문 1:
What would you suggest to obtain a clear solution of it?

답변:
It can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly, while in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml it is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, so it is recommended to prepare the solution just before use.

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