CI994 (Tacedinaline)

Description

Name: CI994 (Tacedinaline)
Brand: Selleckchem
SKU: S2818

Description

CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest. Phase 3.

0.57 μM ^[1]

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]

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]

CI994 (Tacedinaline)

Catalog No.S2818

CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest. Phase 3.

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Cell lines	LNCaP cell lines
Concentrations	2.5 μM
Incubation Time	2-4 days
Method	LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×10⁴) are seeded in 24-well plates and incubated in a 5% CO₂ incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate.

Animal Models	human prostate tumor model LNCaP
Dosages	535 mg/kg
Administration	Administered via oral gavage
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT00005624	Completed	Multiple Myeloma	H. Lee Moffitt Cancer Center and Research Institute\|National Cancer Institute (NCI)\|Parke-Davis	1997-08	Phase 2
NCT00005624	Completed	Multiple Myeloma	H. Lee Moffitt Cancer Center and Research Institute\|National Cancer Institute (NCI)\|Parke-Davis	1997-08	Phase 2
NCT00004861	Completed	Pancreatic Cancer	Pfizer	1999-10	Phase 2
NCT00005093	Completed	Lung Cancer	Pfizer	1999-12	Phase 3

Solubility (25°C) *	In vitro	DMSO	54 mg/mL (200 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.