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CI-994

(CAS No:112522-64-2)

Tacedinaline (CI994) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.

CAS No:112522-64-2

Molecular Weight(MW):269.3

Purity:99.00%

Specification:500MG;1G;5G;10G;50G;100G

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	112522-64-2
Molecular formula(MF)	C₁₅H₁₅N₃O₂
Molecular Weight(MW):	269.3
Alias

Solubility

In vitro	DMSO	54 mg/mL (200.51 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo	5% DMSO+40% PEG 300+ddH2O	5mg/mL

Biological Activity

Description

Tacedinaline (CI994) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.

Targets

HDAC1 ^[1] (Cell-free assay)	HDAC2 ^[1]	HDAC3 ^[1]
0.9 μM	0.9 μM	1.2 μM

In vitro

CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells. ^[2] CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. ^[3] CI-994 exerts activity against several tumor cell lines with greater cytotoxicity against the solid tumors relative to both the leukemia and normal fibroblast cell lines. ^[4] CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. ^[5]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human MDA-MB-231 cells	Growth inhibition assay	5 days	Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay, GI50=0.17 Î¼M	18543902
human PC3 cells	Growth inhibition assay	5 days	Growth inhibition of human PC3 cells after 5 days by MTT assay, GI50=0.29 Î¼M	18543902
human HCT116 cells	CytotoxicÂ assay		Cytotoxicity against human HCT116 cells by MTT assay, IC50=4 Î¼M	17941625
293T cells	Function assay		Inhibition of HDAC in 293T cells, IC50=6 Î¼M	17941625
human LNCap	Proliferation assay		Antiproliferative activity against human LNCap by MTT assayï¼ IC50=7.4 Î¼M	18166465
human NCI-H661 cells	Proliferation assay	48 h	Antiproliferative activity against human NCI-H661 cells after 48 hrs, IC50=20 Î¼M	18692397
human NCI-H661 cells	Function assay	6 h	Inhibition of HDAC in human NCI-H661 cells assessed as histone H4 acetylation after 6 hrs by Western blot analysis	18692397

... Click to View More Cell Line Experimental Data

In vivo

CI-994 exerts demonstrated antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP. ^[4]