Ricolinostat (Synonyms: ACY-1215; Rocilinostat)

目录号: HY-16026 纯度: 99.83%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Ricolinostat (ACY-1215) 是一种有效，选择性的 HDAC6 抑制剂，IC₅₀ 为 5 nM。ACY-1215 也可抑制 HDAC1，HDAC2 和 HDAC3，IC₅₀ 分别为 58，48 和 51 nM。

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Ricolinostat Chemical Structure

CAS No. : 1316214-52-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥715	In-stock
1 mg	￥261	In-stock
5 mg	￥650	In-stock
10 mg	￥990	In-stock
50 mg	￥2800	In-stock
100 mg	￥4850	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

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Customer Review

MCE 顾客使用本产品发表的 30 篇科研文献

: Ricolinostat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jan;109:2464-2471. [Abstract]; The expression of IL-1β and IL-6 in human primary chondrocytes and C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.

: Ricolinostat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jan;109:2464-2471. [Abstract]; The expression of MMP-1, MMP-13 and COL2 A1 in C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.

: Ricolinostat purchased from MCE. Usage Cited in: Oncogene. 2018 Nov;37(45):5952-5966. [Abstract]; Mouse CAFs are treated with increasing concentrations of ACY1215 for 24 h. Western blot analysis of tubulin, histone H3, histone H4, acetylated tubulin, acetylated histone H3, and acetylated histone H4.

: Ricolinostat purchased from MCE. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1270-1276. [Abstract]; A375 cells are treated with indicated concentrations of ACY-1215. After 72 h, Western blotting assay are utilized to detect apoptosis.

: Ricolinostat purchased from MCE. Usage Cited in: Cancer Lett. 2016 Aug 28;379(1):134-142. [Abstract]; Inhibition of HDAC6 by HDAC6-selective inhibitors impairs the proliferation of glioblastoma cells. U87 and U251 cells are treated with HDAC6 selective inhibitors and the cells are harvested for subsequent western blot analysis.

: Ricolinostat purchased from MCE. Usage Cited in: Med Oncol. 2016 May;33(5):50. [Abstract]; H460 cells are treated with 0.5 μM Aorafenib and indicated concentration of HDAC6 inhibitors, CAY10603 (CAY, 0.05 μM) or ACY1215 (ACY,1 μM). The cleavage of PARP and caspase 3 also increased after cotreatment.

Ricolinostat 相关产品

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC₅₀ of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC₅₀s of 58, 48, and 51 nM, respectively.

IC₅₀ & Target^[1]

HDAC6

4.7 nM (IC₅₀)

HDAC2

48 nM (IC₅₀)

HDAC3

51 nM (IC₅₀)

HDAC1

58 nM (IC₅₀)

HDAC8

100 nM (IC₅₀)

HDAC7

1400 nM (IC₅₀)

HDAC5

5000 nM (IC₅₀)

HDAC4

7000 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
697	IC₅₀	201 nM Compound: Ricolinostat	Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay	[PMID: 31710483]
A2780	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay Cytotoxicity against human A2780 cells after 72 hrs by MTT assay	[PMID: 26443078]
A549	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26443078]
A549	IC₅₀	7.7 μM Compound: ACY1215	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 30525585]
HAL-01	IC₅₀	> 25 μM Compound: Ricolinostat	Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
HAL-01	IC₅₀	2.04 μM Compound: Ricolinostat	Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36351184]
HCT-116	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 26443078]
HCT-116	IC₅₀	1.85 μM Compound: ACY-1215	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
HEL	IC₅₀	2.54 μM Compound: 28; ACY1215	Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay	[PMID: 29940115]
HEL	IC₅₀	3.75 μM Compound: 28; ACY1215	Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
HeLa	IC₅₀	> 5000 nM Compound: ACY-1215	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 26443078]
HepG2	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 26443078]
HL-60	IC₅₀	> 10000 nM Compound: Ricolinostat	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 33360560]
HL-60	IC₅₀	1.54 μM Compound: Ricolinostat	Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36351184]
HL-60	IC₅₀	10.37 μM Compound: Ricolinostat	Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
HL-60	IC₅₀	2.36 μM Compound: Ricolinostat	Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
HL-60	IC₅₀	2.54 μM Compound: 28; ACY1215	Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay	[PMID: 29940115]
HL-60	IC₅₀	3.75 μM Compound: 28; ACY1215	Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
HPBALL	IC₅₀	6.7 μM Compound: Ricolinostat	Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
HT-29	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 26443078]
HUVEC	IC₅₀	13.62 μM Compound: ACY-1215	Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
Jurkat	IC₅₀	2.42 μM Compound: Ricolinostat	Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 36351184]
K562	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 26443078]
K562	IC₅₀	2.54 μM Compound: 28; ACY1215	Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay	[PMID: 29940115]
K562	IC₅₀	3.75 μM Compound: 28; ACY1215	Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
K562	IC₅₀	6.02 μM Compound: Ricolinostat	Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
KCL-22	IC₅₀	3.38 μM Compound: Ricolinostat	Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
KCL-22	IC₅₀	3.75 μM Compound: Ricolinostat	Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
KM12	IC₅₀	2.15 μM Compound: ACY-1215	Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
MM1.S	IC₅₀	0.84 μM Compound: ACY-1215	Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
MM1.S	EC₅₀	0.85 nM Compound: ACY-1215	Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs	[PMID: 33359604]
MM1.S	IC₅₀	2 μM Compound: 18; ACY-1215	Cytotoxicity against human MM1.S cells incubated for 48 hrs by MTT assay Cytotoxicity against human MM1.S cells incubated for 48 hrs by MTT assay	[PMID: 29133060]
MV4-11	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 26443078]
MV4-11	IC₅₀	0.656 μM Compound: 5	Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MV4-11	IC₅₀	0.656 μM Compound: ACY-1215	Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
MV4-11	IC₅₀	0.81 μM Compound: ACY-1215	Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
NCI-H460	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 26443078]
NCI-H929	GI₅₀	> 100 μM Compound: 3; ACY-1215	Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay	[PMID: 29304284]
OPM-2	IC₅₀	2 μM Compound: 18; ACY-1215	Cytotoxicity against human OPM-2 cells incubated for 48 hrs by MTT assay Cytotoxicity against human OPM-2 cells incubated for 48 hrs by MTT assay	[PMID: 29133060]
PBMC	IC₅₀	< 3.6 μM Compound: Ricolinostat	Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
Ramos	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human Ramos cells after 72 hrs by MTT assay Cytotoxicity against human Ramos cells after 72 hrs by MTT assay	[PMID: 26443078]
REH	IC₅₀	> 25 μM Compound: Ricolinostat	Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
RPMI-8226	IC₅₀	11 μM Compound: ACY-1215	Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 30594434]
RPMI-8226	IC₅₀	1468 nM Compound: ACY-1215	Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 26443078]
RPMI-8226	GI₅₀	6.4 μM Compound: 3; ACY-1215	Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay	[PMID: 29304284]
RPMI-8226	IC₅₀	9.26 μM Compound: ACY-1215	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay	[PMID: 31865013]
SEM	IC₅₀	1.61 μM Compound: Ricolinostat	Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
Sf9	IC₅₀	> 1 μM Compound: ACY1215	Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.379 μM Compound: ACY1215	Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	12 nM Compound: Ricolinostat	Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method	[PMID: 31710483]
Sf9	IC₅₀	4.7 nM Compound: ACY-1215	Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a	[PMID: 31414801]
Sf9	IC₅₀	5 nM Compound: ACY-1215	Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay	[PMID: 30594434]
Sf9	IC₅₀	58 nM Compound: ACY-1215	Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr	[PMID: 31414801]
Sf9	IC₅₀	74 nM Compound: ACY-1215	Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay	[PMID: 30594434]
SK-BR-3	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay	[PMID: 26443078]
SK-OV-3	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 26443078]
SU-DHL-6	IC₅₀	0.83 μM Compound: ACY-1215	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
SUP-B15	IC₅₀	1.92 μM Compound: Ricolinostat	Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
SUP-B15	IC₅₀	3.54 μM Compound: Ricolinostat	Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]
T47D	IC₅₀	0.71 μM Compound: ACY-1215	Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
TALL-1	IC₅₀	3.88 μM Compound: Ricolinostat	Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay	[PMID: 34582215]
U-266	IC₅₀	> 100 μM Compound: ACY-1215	Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay	[PMID: 31865013]
U-266	GI₅₀	> 100 μM Compound: 3; ACY-1215	Antiproliferative activity against human U266 cells after 48 hrs by SRB assay Antiproliferative activity against human U266 cells after 48 hrs by SRB assay	[PMID: 29304284]
U-266	IC₅₀	> 5000 nM Compound: ACY-1215	Cytotoxicity against human U266 cells after 72 hrs by MTT assay Cytotoxicity against human U266 cells after 72 hrs by MTT assay	[PMID: 26443078]
U-266	IC₅₀	21.2 μM Compound: ACY-1215	Growth inhibition of human U266 cells after 72 hrs by MTT assay Growth inhibition of human U266 cells after 72 hrs by MTT assay	[PMID: 30594434]
U-266	IC₅₀	3.52 μM Compound: Ricolinostat	Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30365892]

体外研究
(In Vitro)

Ricolinostat (ACY-1215) 对 HDAC8 具有轻微活性 (IC₅₀=0.1 μM) ，对 HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1 和 Sirtuin2 的活性较低 (IC₅₀>1 μM) 。在多发性骨髓瘤 (MM) 细胞系中表现出剂量依赖性细胞活力降低，IC₅₀ 范围为 2-8 μM；对 PS-341 耐药 MM 细胞系 (ANBL-6.BR) 显示显著活性，表明其可克服 PS-341 的耐药性^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

接受 Ricolinostat (ACY-1215)、PS-341 或 Ricolinostat 加 PS-341 治疗的小鼠的肿瘤生长明显延迟(分别为 P=0.01、P=0.006 和 P<0.0001)。与对照组(对照组 17 天 vs 联合治疗组 40 天，P<0.0001)和 Ricolinostat (ACY-1215) 治疗组(PS-341 组 22 天 vs 联合治疗组 40 天，P<0.0001)相比，Ricolinostat 和 PS-341 联合治疗可显著抑制肿瘤生长并显著延长总生存期 (OS)。与治疗期间同一天的对照组值相比，联合治疗组的体重减轻在 4% 至 12% 之间，最后一次注射后完全恢复。在浆细胞瘤模型中观察到，Ricolinostat 与 PS-341 联合使用与单独使用任一药物相比具有显著的治疗优势^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

433.50

Formula

C₂₄H₂₇N₅O₃

CAS 号

1316214-52-4

性状

固体

颜色

White to pink

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 50 mg/mL (115.34 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3068 mL	11.5340 mL	23.0681 mL
5 mM	0.4614 mL	2.3068 mL	4.6136 mL
10 mM	0.2307 mL	1.1534 mL	2.3068 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.77 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.77 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.77 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.83%

选择批次：

Data Sheet (643 KB) SDS (393 KB)

COA (188 KB) LCMS (262 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Santo L, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with PS-341 in multiple myeloma. Blood. 2012 Mar 15;119(11):2579-89. [Content Brief]

Cell Assay ^[1]	The effect of Ricolinostat with or without PS-341 on the viability of MM cell lines, patient MM cells, and PBMCs is assessed by measuring MTT dye absorbance. PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of Ricolinostat (ACY-1215). DNA synthesis is measured by tritiated thymidine uptake. CD4⁺ T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3×10⁴ cells/well) are incubated in 96-well culture plates with medium and different concentrations of Ricolinostat (ACY-1215), PS-341, and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] To evaluate the in vivo anti-MM activity of Ricolinostat, male SCID mice are inoculated subcutaneously with 5×10⁶ MM.1S cells in 100 μL of serum-free RPMI 1640 medium. When tumors are measurable, mice are treated IP with Ricolinostat 50 mg/kg dissolved in 10% DMSO in 5% dextrose in water consecutively for 5 days a week for 3 weeks; PS-341 0.5 mg/kg dissolved in 0.9% saline solution biweekly (IV) for 3 consecutive weeks; or combination with the same dosing regimen used for the individual agents. The control group receive the carrier alone at the same schedule as the combination group. Tumor size is measured every other day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V=0.5(a×b²) where a is the long diameter of the tumor and b is the short diameter of the tumor. Mice are killed when the tumor reaches 2 cm³ or is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Santo L, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with PS-341 in multiple myeloma. Blood. 2012 Mar 15;119(11):2579-89. [Content Brief]

Ricolinostat 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3068 mL	11.5340 mL	23.0681 mL	57.6701 mL
	5 mM	0.4614 mL	2.3068 mL	4.6136 mL	11.5340 mL
	10 mM	0.2307 mL	1.1534 mL	2.3068 mL	5.7670 mL
	15 mM	0.1538 mL	0.7689 mL	1.5379 mL	3.8447 mL
	20 mM	0.1153 mL	0.5767 mL	1.1534 mL	2.8835 mL
	25 mM	0.0923 mL	0.4614 mL	0.9227 mL	2.3068 mL
	30 mM	0.0769 mL	0.3845 mL	0.7689 mL	1.9223 mL
	40 mM	0.0577 mL	0.2884 mL	0.5767 mL	1.4418 mL
	50 mM	0.0461 mL	0.2307 mL	0.4614 mL	1.1534 mL
	60 mM	0.0384 mL	0.1922 mL	0.3845 mL	0.9612 mL
	80 mM	0.0288 mL	0.1442 mL	0.2884 mL	0.7209 mL
	100 mM	0.0231 mL	0.1153 mL	0.2307 mL	0.5767 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ricolinostat1316214-52-4ACY-1215 RocilinostatACY1215ACY 1215HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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Ricolinostat (Synonyms: ACY-1215; Rocilinostat)

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Ricolinostat (Synonyms: ACY-1215; Rocilinostat)

Customer Review

Ricolinostat 相关抗体

MCE 顾客使用本产品发表的 30 篇科研文献

Ricolinostat 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HDAC 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Ricolinostat 相关抗体:

摩尔计算器

稀释计算器

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完整储备液配制表

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