C0621
CI−994
≥98% (HPLC), HDAC Inhibitor, powder
Synonyme(s) :
4-Acetylamino-N-(2′-aminophenyl)benzamide, Acetyldinaline, Tacedinaline
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A propos de cet article
Formule empirique (notation de Hill) :
C15H15N3O2
Numéro CAS:
Poids moléculaire :
269.30
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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Laissez-nous vous aiderNom du produit
CI−994, ≥98% (HPLC), powder
SMILES string
CC(=O)Nc1ccc(cc1)C(=O)Nc2ccccc2N
InChI key
VAZAPHZUAVEOMC-UHFFFAOYSA-N
InChI
1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20)
assay
≥98% (HPLC)
form
powder
color
off-white
solubility
DMSO: >10 mg/mL
storage temp.
room temp
Quality Level
Gene Information
Catégories apparentées
Application
CI-994 has been used:
- as an histone deacetylase (HDAC) inhibitor to treat SUM229 and DT22 cells to study its effects
- as an HDAC inhibitor for screening in SPEL cells
- to study its effects on human myeloid and erythroid progenitors
Biochem/physiol Actions
CI-994 is the acetylated derivative form of the original compound Dinaline (PD 104 208). It is an oral cytostatic drug with impressive differential activity against leukemic cells & normal stem-cells. It is used for combination therapy for selected tumors including non-small cell lung, pancreatic, breast, and colorectal cancers. It acts as a histone deacetylase inhibitor. CI-994 blocks cells in the G1-S phase of the cell cycle. The 16 kDa phosphoprotein is confined to the nuclear compartment. Loss of the 16-kDa nuclear phosphoprotein appears to be a direct effect of CI-994 treatment and that the inhibition of this phosphoprotein may play a critical role in the mechanism of action of CI-994.
Orally available HDAC Inhibitor; CI-994 blocks cells in the G1-S phase of the cell cycle.
Features and Benefits
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Warning
hcodes
Hazard Classifications
Eye Irrit. 2
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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S D Undevia et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 15(11), 1705-1711 (2004-11-03)
This study was conducted to determine the toxicity profile, maximum tolerated dose (MTD) and pharmacokinetics of the putative histone deacetylase inhibitor CI-994 in combination with capecitabine. Fifty-four patients were treated according to three different dosing schemes in which the capecitabine
Ekaterina P Mochalova et al.
Scientific reports, 9(1), 10263-10263 (2019-07-18)
It is known that MuRF-1 and atrogin-1/MAFbx mRNA expression is increased in rat soleus muscle under unloading conditions. We aimed to determine the role of histone deacetylase 1 (HDAC1) in the activation of MuRF-1 and MAFbx expression in rat soleus
Suxiang Zhang et al.
Cell death & disease, 9(5), 460-460 (2018-04-28)
Spinal cord injury (SCI) induces severe and long-lasting neurological disability. Accumulating evidence has suggested that histone deacetylase (HDAC) inhibitors exert neuroprotective effects against various insults and deficits in the central nervous system. In the present study, we assessed the effect
S Prakash et al.
Investigational new drugs, 19(1), 1-11 (2001-04-09)
CI-994 (N-acetyl dinaline, PD 123654) is a novel oral agent active in a broad variety of murine and human tumor xenografts. While cytotoxic in the Brown Norway (BN) rat leukemia model, growth inhibition in other murine and human tumor xenografts
P M LoRusso et al.
Investigational new drugs, 14(4), 349-356 (1996-01-01)
CI-994 [aka: acetyldinaline; PD 123654; 4-acetylamino-N-(2'aminophenyl)-benzamide] (Figure 1) is a novel antitumor agent with a unique mechanism of action. It is the acetylated metabolite of dinaline, a compound previously identified as having cytotoxic and cytostatic activity against several murine and
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