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C0621

Sigma-Aldrich

CI−994

≥98% (HPLC), powder

Sinónimos:

4-Acetylamino-N-(2′-aminophenyl)benzamide, Acetyldinaline, Tacedinaline

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About This Item

Fórmula empírica (notación de Hill):
C15H15N3O2
Número de CAS:
112522-64-2
Peso molecular:
269.30
Número MDL:
MFCD00866266
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
329774808
NACRES:
NA.77

Nivel de calidad

100

Análisis

≥98% (HPLC)

formulario

powder

color

off-white

solubilidad

DMSO: >10 mg/mL

temp. de almacenamiento

room temp

cadena SMILES

CC(=O)Nc1ccc(cc1)C(=O)Nc2ccccc2N

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)

Clave InChI

VAZAPHZUAVEOMC-UHFFFAOYSA-N

Información sobre el gen

human ... HDAC1(3065) , HDAC10(83933) , HDAC11(79885) , HDAC2(3066) , HDAC3(8841) , HDAC4(9759) , HDAC5(10014) , HDAC6(10013) , HDAC7(51564) , HDAC8(55869) , HDAC9(9734)

Aplicación

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

Acciones bioquímicas o fisiológicas

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.

Características y beneficios

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Pictogramas

Exclamation mark
GHS07

Palabra de señalización

Warning

Frases de peligro

H319

Clasificaciones de peligro

Eye Irrit. 2

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Equipo de protección personal

dust mask type N95 (US), Eyeshields, Gloves

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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CoREST Complex-Selective Histone Deacetylase Inhibitors Show Prosynaptic Effects and an Improved Safety Profile To Enable Treatment of Synaptopathies
Fuller NO, et al.
ACS Chemical Neuroscience (2019)
D A Richards et al.
Annals of oncology : official journal of the European Society for Medical Oncology, 17(7), 1096-1102 (2006-04-28)
CI-994, an oral histone deacetylase inhibitor, has antineoplastic activity and synergism with gemcitabine preclinically. This randomized phase II trial explored whether CI-994 plus gemcitabine improves overall survival, objective response, duration of response, time to treatment failure and change in quality
M H Seelig et al.
European journal of cancer (Oxford, England : 1990), 32A(11), 1968-1976 (1996-10-01)
Dinaline [4-amino-N-(2'-aminophenyl)-benzamide, Din], p-N-methyldinaline (Me-Din) and p-N-acetyldinaline (Ac-Din) were evaluated for their antineoplastic efficacy in acetoxymethylmethylnitrosamine-induced colorectal carcinomas in Sprague-Dawley rats and in two human colon cancer cell lines. Din was very effective at all dosages (10, 7.7 and 5.9
H M el-Beltagi et al.
Leukemia, 7(11), 1795-1800 (1993-11-01)
The efficacy of acetyldinaline [4-acetylamino-N-(2'-aminophenyl)-benzamide] for eradication of minimal residual disease (MRD), which is left after bone marrow transplantation, and the risk of a bone marrow graft being jeopardized by this treatment was studied in the Brown Norway rat acute
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
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