MS-275 CAS: 209783-80-2
MF: C21H20N4O3
MW: 376.41
An HDAC inhibitor shown to inhibit angiogenesis and metastasis.

MS-275 (CAS 209783-80-2)

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MS-275 is rated 5.0 out of 5 by 2.
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Nombres Alternativos: Entinostat
Solicitud: MS-275 is an HDAC inhibitor shown to inhibit angiogenesis and metastasis
Número de CAS: 209783-80-2
Pureza: ≥98%
Peso Molecular: 376.41
Fórmula Molecular: C21H20N4O3
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
* En el Certificado de Análisis específico de lote, puede encontrar información específica (como el contenido en agua).

MS-275 is an inhibitor of HDAC (histone deacetylase) that preferentially inhibits HDAC1 (IC50 = 300 nM) over HDAC3 (IC50 = 8 μM). However, MS-275 does not inhibit HDAC8 (IC50 > 100 μM). MS-275 induces cyclin-dependent kinase inhibitor 1A (p21/CIP1/WAF1), slowing cell growth, differentiation, and tumor development in vivo. Recent studies suggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drugs, like adriamycin, inhibitors of poly (ADP-ribose) polymerase (PARP), or inhibitors of heat shock protein 90 (Hsp90).


References

1 Hu, E., Dul, E., Sung, C., et al. Identification of novel isoform-selective inhibitors within class I histone deacetylases. J Pharmacol Exp Ther 307 720-728 (2003). 2 Saito, A., Yamashita, T., Mariko, Y., et al. A synthetic inhibitor of histone deacetylase, MS-27-275, with marked in vivo antitumor activity against human tumors. Proc Natl Acad Sci USA 96 4592-4597 (1999). 3 Jaboin, J., Wild, J., Hamidi, H., et al. MS-27-275, an inhibitor of histone deacetylase, has marked in vitro and in vivo antitumor activity against pediatric solid tumors. Cancer Res 62 6108-6115 (2002). 4 Xu, J., Zhou, J., Wei, W., et al. Sp1-mediated TRAIL induction in chemosensitization. Cancer Res 68(16) 6718-6726 (2008). 5 Gaymes, T.J., Shall, S., Macpherson, L.J., et al. Inhibitors of poly ADP-ribose polymerase (PARP) induce apoptosis of myeloid leukemic cells: potential for therapy of myeloid leukemia and myelodysplastic syndromes. Haematologica 94 638-646 (2009). 6 Nguyen, A., Su, L., Campbell, B., et al. Synergism of heat shock protein 90 and histone deacetylase inhibitors in synovial sarcoma. Sarcoma (2009).

Apariencia :
Crystalline or powder
Estado de Materia :
Solid
Solubilidad :
Soluble in methanol, DMSO (~30 mg/ml), DMF (~30 mg/ml), ethanol (~2 mg/ml), 1:1 solution of DMSO:PBS(PH7.2) (~0.5 mg/ml), and water (<1 mg/ml) at 25° C.
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
158-160° C
Punto de ebullición :
566.74° C at 760 mmHg (Predicted)
Densidad :
1.32 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.67 (Predicted)
IC50 :
HDAC1: IC50 = 300 nM; HDAC3: IC50 = 1.7 µM; HepG2 : IC50 = 0.9 nM (human); Histone deacetylase 1: IC50 = 110 nM (human); Histone deacetylase 2: IC50 = 15 nM (human)
Datos Ki :
Histone deacetylase 1: Ki= 22 nM (human); Histone deacetylase 2: Ki= 65 nM (human); Histone deacetylase 3: Ki= 360 nM (human); Histone deacetylase-like amidohydrolase: Ki= >100 µM (Alcaligenes sp)
Valores de pK :
pKa: 11.32 (Predicted), pKb: 4.32 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
WGK Alemania :
3
PubChem CID :
4261
Número MDL :
MFCD08272435
SMILES :
C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3

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PMID: # 31308194  Dedoni, S.|Marras, L.|Olianas, MC.|Ingianni, A.|Onali, PL.| et al. 2019. J. Pharmacol. Exp. Ther. 370: 490-503.

PMID: # 30617154  Westergard, T.|McAvoy, K.|Russell, K.|Wen, X.|Pang, Y.|Morris, B.|Pasinelli, P.|Trotti, D.|Haeusler, A.| et al. 2019. EMBO Mol Med. 11:

PMID: # 29235036  Ho, CF.|Bon, CP.|Ng, YK.|Herr, DR.|Wu, JS.|Lin, TN.|Ong, WY.| et al. 2018. Neurochem. Res. 43: 540-555.

PMID: # 29074567  Gendarme, M. et al. 2017. Mol. Biol. Cell.

PMID: # 27362706  Kang, SH. et al. 2016. Clin. Exp. Pharmacol. Physiol. 43: 995-1003.

PMID: # 27319010  2016. Neuromolecular Med.

PMID: # 25808664  Esrick, EB. et al. 2015. American journal of hematology. 90: 624-8.

PMID: # 26162318  Tan, CS. et al. 2015. Molecular neurobiology.

PMID: # 22341874  Lin, H. et al. 2012. Brain Res. 1447: 119-125.

PMID: # 22422937  Pazolli, E. et al. 2012. Cancer research. 72: 2251-61.

Citaciones 1 a 10 de un total de 15
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