Citarinostat (Synonyms: ACY241)

Name: Citarinostat
Brand: MedChemExpress
SKU: HY-15994
Rating: 5.0 (3 reviews)

Cat. No.: HY-15994 Purity: 99.55%: Data Sheet
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Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC₅₀ of 2.6 nM (IC₅₀s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects.

For research use only. We do not sell to patients.

Citarinostat Chemical Structure

CAS No. : 1316215-12-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE Citarinostat

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HDAC Isoform Specific Products:

View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HDAC6

2.6 nM (IC₅₀)

HDAC1

35 nM (IC₅₀)

HDAC2

45 nM (IC₅₀)

HDAC3

46 nM (IC₅₀)

HDAC8

137 nM (IC₅₀)

HDAC7

7300 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BV-173	IC₅₀	0.9 3 Compound: Citarinostat	Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
BV-173	IC₅₀	0.9 3 Compound: Citarinostat	Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
BV-173	IC₅₀	0.9 3 Compound: Citarinostat	Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Fibroblast	IC₅₀	5.7 3 Compound: 6	Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	5.7 3 Compound: 6	Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Sf9	IC₅₀	2.6 1 Compound: ACY-241	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]
Fibroblast	IC₅₀	5.7 3 Compound: ACY-241	Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	5.7 3 Compound: 6	Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	5.7 3 Compound: ACY-241	Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	5.74 3 Compound: ACY-241	Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Fibroblast	IC₅₀	5.74 3 Compound: ACY-241	Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Fibroblast	IC₅₀	5.74 3 Compound: ACY-241	Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Fibroblast	IC₅₀	7.4 3 Compound: 6	Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	7.4 3 Compound: 6	Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	7.4 3 Compound: ACY-241	Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	7.4 3 Compound: ACY-241	Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	7.4 3 Compound: ACY-241	Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Fibroblast	IC₅₀	7.4 3 Compound: 6	Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Fibroblast	IC₅₀	7.44 3 Compound: ACY-241	Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Fibroblast	IC₅₀	7.44 3 Compound: ACY-241	Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Fibroblast	IC₅₀	5.7 3 Compound: ACY-241	Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
HeLa	IC₅₀	7 3 Compound: Citarinostat	Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Fibroblast	IC₅₀	7.44 3 Compound: ACY-241	Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HUVEC	IC₅₀	4.86 3 Compound: ACY-241	Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HUVEC	IC₅₀	4.9 3 Compound: 6	Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
HuT78	IC₅₀	1.78 3 Compound: ACY-241	Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HeLa	IC₅₀	7 3 Compound: Citarinostat	Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
HUVEC	IC₅₀	4.9 3 Compound: ACY-241	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
HUVEC	IC₅₀	4.86 3 Compound: ACY-241	Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HuT78	IC₅₀	1.78 3 Compound: ACY-241	Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HUVEC	IC₅₀	4.9 3 Compound: 6	Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
HUVEC	IC₅₀	4.86 3 Compound: ACY-241	Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
HeLa	IC₅₀	7 3 Compound: Citarinostat	Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
HUVEC	IC₅₀	4.9 3 Compound: ACY-241	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
HUVEC	IC₅₀	4.9 3 Compound: 6	Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
HuT78	IC₅₀	1.78 3 Compound: ACY-241	Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Jurkat	IC₅₀	1.2 3 Compound: Citarinostat	Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
HUVEC	IC₅₀	4.9 3 Compound: ACY-241	Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
MM1.S	IC₅₀	1.52 3 Compound: 6	Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Jurkat	IC₅₀	1.2 3 Compound: Citarinostat	Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Jurkat	IC₅₀	1.2 3 Compound: Citarinostat	Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
L02	IC₅₀	15.2 3 Compound: ACY-241	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay	[PMID: 37463038]
MM1.S	IC₅₀	1.6 3 Compound: Citarinostat	Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Sf9	IC₅₀	35 1 Compound: ACY-241	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]
MM1.S	IC₅₀	1.52 3 Compound: 6	Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MM1.S	IC₅₀	1.61 3 Compound: ACY-241	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	IC₅₀	1.6 3 Compound: Citarinostat	Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MM1.S	IC₅₀	1.6 3 Compound: Citarinostat	Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MOLM-13	IC₅₀	13.5 3 Compound: Citarinostat	Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MM1.S	IC₅₀	1.61 3 Compound: ACY-241	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]
MOLT-4	IC₅₀	1.72 3 Compound: ACY-241	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
MM1.S	IC₅₀	2 3 Compound: ACY-241	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay	[PMID: 37463038]
MM1.S	IC₅₀	2 3 Compound: ACY-241	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay	[PMID: 37463038]
MV4-11	IC₅₀	1.2 3 Compound: Citarinostat	Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MM1.S	IC₅₀	1.61 3 Compound: ACY-241	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]
MV4-11	IC₅₀	1.24 3 Compound: 6	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]
MM1.S	IC₅₀	1.52 3 Compound: 6	Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MOLM-13	IC₅₀	13.5 3 Compound: Citarinostat	Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MV4-11	IC₅₀	1.24 3 Compound: ACY-241	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]
MOLM-13	IC₅₀	13.5 3 Compound: Citarinostat	Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MOLT-4	IC₅₀	1.72 3 Compound: ACY-241	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
MV4-11	IC₅₀	1.34 3 Compound: ACY-241	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]
MOLT-4	IC₅₀	1.72 3 Compound: ACY-241	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
MV4-11	IC₅₀	1.34 3 Compound: ACY-241	Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
MV4-11	IC₅₀	1.2 3 Compound: Citarinostat	Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
NSC	IC₅₀	4.35 3 Compound: ACY-241	Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
MV4-11	IC₅₀	1.34 3 Compound: ACY-241	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]
OCI-AML-3	IC₅₀	7.7 3 Compound: Citarinostat	Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MV4-11	IC₅₀	1.24 3 Compound: ACY-241	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]
RPMI-8226	IC₅₀	3.16 3 Compound: 6	Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
MV4-11	IC₅₀	1.24 3 Compound: 6	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]
RPMI-8226	IC₅₀	6.5 3 Compound: Citarinostat	Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
NSC	IC₅₀	4.35 3 Compound: ACY-241	Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
Sf9	IC₅₀	> 1 3 Compound: Citarinostat	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]
OCI-AML-3	IC₅₀	7.7 3 Compound: Citarinostat	Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Sf9	IC₅₀	0.318 3 Compound: Citarinostat	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]
RPMI-8226	IC₅₀	6.5 3 Compound: Citarinostat	Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Sf9	IC₅₀	2.6 1 Compound: ACY-241	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]
RPMI-8226	IC₅₀	3.5 3 Compound: ACY-241	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay	[PMID: 37463038]
RPMI-8226	IC₅₀	3.16 3 Compound: 6	Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
Sf9	IC₅₀	35 1 Compound: ACY-241	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]
SU-DHL-1	IC₅₀	4.56 3 Compound: ACY-241	Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Sf9	IC₅₀	0.318 3 Compound: Citarinostat	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]
U-87MG ATCC	IC₅₀	9.1 3 Compound: Citarinostat	Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
Sf9	IC₅₀	>1 3 Compound: Citarinostat	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]
SU-DHL-1	IC₅₀	4.56 3 Compound: ACY-241	Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
U-87MG ATCC	IC₅₀	9.1 3 Compound: Citarinostat	Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MV4-11	IC₅₀	1.2 3 Compound: Citarinostat	Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
MV4-11	IC₅₀	1.24 3 Compound: 6	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	1.24 3 Compound: ACY-241	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	1.34 3 Compound: ACY-241	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]
MV4-11	IC₅₀	1.34 3 Compound: ACY-241	Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
NSC	IC₅₀	4.35 3 Compound: ACY-241	Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis	[PMID: 35119267]
OCI-AML-3	IC₅₀	7.7 3 Compound: Citarinostat	Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
RPMI-8226	IC₅₀	3.16 3 Compound: 6	Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method	[PMID: 32615502]
RPMI-8226	IC₅₀	3.5 3 Compound: ACY-241	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay	[PMID: 37463038]
RPMI-8226	IC₅₀	6.5 3 Compound: Citarinostat	Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]
SU-DHL-1	IC₅₀	4.56 3 Compound: ACY-241	Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay	[PMID: 34101461]
Sf9	IC₅₀	0.318 3 Compound: Citarinostat	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	2.6 1 Compound: ACY-241	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	35 1 Compound: ACY-241	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	> 1 3 Compound: Citarinostat	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]
U-266	IC₅₀	4.3 3 Compound: ACY-241	Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay	[PMID: 37463038]
U-87MG ATCC	IC₅₀	9.1 3 Compound: Citarinostat	Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay	[PMID: 33576627]

In Vitro

Citarinostat (ACY241; 0-3 μM; 24 hours; A2780 cells) treatment with 300 nM results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, is only observed at doses above 1 μM. Low exposures of Citarinostat result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes^[1].
The single agent viability IC₅₀ of Citarinostat (ACY241) ranged from 4.6-6.1 μM in A2780 and TOV-21G ovarian cancer and MDA-MD-231 breast cancer cells. Consistent with the viability assay, single agent Citarinostat modestly reduces proliferation at doses up to 3 μM without inducing apoptosis, while 10 μM of Citarinostat causes significant induction of apoptosis and completely suppresses proliferation^[1].

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

Western Blot Analysis^[1]

Cell Line:	A2780 cells
Concentration:	0 μM, 0.1 μM, 0.3 μM, 0.5μM, 1 μM, 3 μM
Incubation Time:	24 hours
Result:	Resulted in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, was only observed at doses above 1 μM.

In Vivo

Citarinostat (ACY241; 50 mg/kg; intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks; female athymic nude mice) significantly suppresses tumor growth in combination with NSC 125973^[1].

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

Animal Model:	Female athymic nude mice (7-week-old) injected with TOV-21G cells^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks
Result:	Combination treatment with NSC 125973 resulted in significantly suppression of tumor growth.

Clinical Trial

Molecular Weight

467.95

Formula

C₂₄H₂₆ClN₅O₃

CAS No.

1316215-12-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (213.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1370 mL	10.6849 mL	21.3698 mL
5 mM	0.4274 mL	2.1370 mL	4.2740 mL
10 mM	0.2137 mL	1.0685 mL	2.1370 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.55%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (244 KB) HNMR (228 KB) RP-HPLC (256 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Huang P, et al. Selective HDAC inhibition by ACY-241 enhances the activity of NSC 125973 in solid tumor models. Oncotarget. 2017 Jan 10;8(2):2694-2707. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1370 mL	10.6849 mL	21.3698 mL	53.4245 mL
	5 mM	0.4274 mL	2.1370 mL	4.2740 mL	10.6849 mL
	10 mM	0.2137 mL	1.0685 mL	2.1370 mL	5.3425 mL
	15 mM	0.1425 mL	0.7123 mL	1.4247 mL	3.5616 mL
	20 mM	0.1068 mL	0.5342 mL	1.0685 mL	2.6712 mL
	25 mM	0.0855 mL	0.4274 mL	0.8548 mL	2.1370 mL
	30 mM	0.0712 mL	0.3562 mL	0.7123 mL	1.7808 mL
	40 mM	0.0534 mL	0.2671 mL	0.5342 mL	1.3356 mL
	50 mM	0.0427 mL	0.2137 mL	0.4274 mL	1.0685 mL
	60 mM	0.0356 mL	0.1781 mL	0.3562 mL	0.8904 mL
	80 mM	0.0267 mL	0.1336 mL	0.2671 mL	0.6678 mL
	100 mM	0.0214 mL	0.1068 mL	0.2137 mL	0.5342 mL

Citarinostat Related Classifications

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:

Citarinostat1316215-12-9ACY241ACY 241ACY-241HDACHistone deacetylasesHDAC6anticanceranti-proliferationα-tubulincombinationmultiple. myelomaInhibitorinhibitorinhibit

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Citarinostat (Synonyms: ACY241)

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