| 词条 | Entinostat |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 444340516 | ImageFile=Entinostat.svg | ImageSize=260 | IUPACName=Pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl] | OtherNames=SNDX-275; MS-275 |Section1={{Chembox Identifiers | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 1ZNY4FKK9H | IUPHAR_ligand = 7007 | CASNo_Ref = {{cascite|correct|??}} | CASNo=209783-80-2 | PubChem=4261 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D09338 | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 132082 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 27759 | SMILES=C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 4111 | InChI = 1/C21H20N4O3/c22-18-5-1-2-6-19(18)25-20(26)17-9-7-15(8-10-17)13-24-21(27)28-14-16-4-3-11-23-12-16/h1-12H,13-14,22H2,(H,24,27)(H,25,26) | InChIKey = INVTYAOGFAGBOE-UHFFFAOYAU | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C21H20N4O3/c22-18-5-1-2-6-19(18)25-20(26)17-9-7-15(8-10-17)13-24-21(27)28-14-16-4-3-11-23-12-16/h1-12H,13-14,22H2,(H,24,27)(H,25,26) | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = INVTYAOGFAGBOE-UHFFFAOYSA-N |Section2={{Chembox Properties | Formula=C21H20N4O3 | MolarMass=376.4085 g/mol | Appearance= | Density= | MeltingPt= | BoilingPt= | Solubility= |Section3={{Chembox Hazards | MainHazards= | FlashPt= | AutoignitionPt = }}Entinostat, also known as SNDX-275 and MS-275, is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers.[1] Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively.[2] Syndax pharmaceuticals currently holds the rights to Entinostat and recently received $26.6 million in funds to advance treatments of resistant cancers using epigenetic tools.[3] Clinical trialsThere is an ongoing phase II trial studying the effect of entinostat on Hodgkin's lymphoma.[4] In 2013, the US FDA granted it breakthrough therapy status for advanced breast cancer. Entinostat is being studied as a treatment for several other cancers, including rhabdomyosarcoma, a difficult-to-treat childhood soft tissue tumor. Narendra Bharathy and Charles Keller at the Children’s Cancer Therapy Development Institute, Oregon, USA investigated why the histone deacetylase inhibitor, entinostat shows promise in treating alveolar rhabdomyosarcoma subtype. Entinostat altered epigenetic regulation to inhibit a fusion protein, PAX3:FOXO1 generated by a chromosomal abnormality driving chemoresistance and aggressive progression. Bharathy et al. showed that in the absence of the fusion protein, rhabdomyosarcoma growth in mouse models slowed, and tumors were sensitized to the chemotherapeutic drug vincristine [5] In preclinical studies, entinostat has also demonstrated synergistic anti-tumor activity in combination with immune checkpoint inhibitors, which may increase the ability of the immune system to attack a range of other tumors.[6] References1. ^Phase I trial of 5-azacitidine (5AC) and SNDX-275 in advanced lung cancer (NSCLC) {{HDAC inhibitors}}{{antineoplastic-drug-stub}}2. ^Novel Sulphonylpyrroles as Inhibitors of Hdac S Novel Sulphonylpyrroles 3. ^http://www.syndax.com/assets/130827%20Syndax%20Series%20B%20news%20release.pdf 4. ^A Phase 2 Multi-Center Study of Entinostat (SNDX-275) in Patient With Relapsed or Refractory Hodgkin's Lymphoma 5. ^{{cite journal | doi = 10.1126/scisignal.aau7632 | pmid = 30459282 | title = The HDAC3–SMARCA4–miR-27a axis promotes expression of the PAX3:FOXO1 fusion oncogene in rhabdomyosarcoma | journal = Science Signaling | volume = 11 | issue = 557 | pages = eaau7632 | year = 2018 | last1 = Bharathy | first1 = Narendra | last2 = Berlow | first2 = Noah E. | last3 = Wang | first3 = Eric | last4 = Abraham | first4 = Jinu | last5 = Settelmeyer | first5 = Teagan P. | last6 = Hooper | first6 = Jody E. | last7 = Svalina | first7 = Matthew N. | last8 = Ishikawa | first8 = Yoshihiro | last9 = Zientek | first9 = Keith | last10 = Bajwa | first10 = Zia | last11 = Goros | first11 = Martin W. | last12 = Hernandez | first12 = Brian S. | last13 = Wolff | first13 = Johannes E. | last14 = Rudek | first14 = Michelle A. | last15 = Xu | first15 = Linping | last16 = Anders | first16 = Nicole M. | last17 = Pal | first17 = Ranadip | last18 = Harrold | first18 = Alexandria P. | last19 = Davies | first19 = Angela M. | last20 = Ashok | first20 = Arya | last21 = Bushby | first21 = Darnell | last22 = Mancini | first22 = Maria | last23 = Noakes | first23 = Christopher | last24 = Goodwin | first24 = Neal C. | last25 = Ordentlich | first25 = Peter | last26 = Keck | first26 = James | last27 = Hawkins | first27 = Douglas S. | last28 = Rudzinski | first28 = Erin R. | last29 = Chatterjee | first29 = Bishwanath | last30 = Bächinger | first30 = Hans Peter | displayauthors = 29 }} 6. ^{{cite web | url = http://www.syndax.com/pipeline/entinostat/ | title = Entinostat | publisher = Syndax | access-date = December 2, 2018}} 4 : Benzamides|Carbamates|Histone deacetylase inhibitors|Pyridines |
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