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恩替诺特 (MS-275)

HDAC1和HDAC3抑制剂

规格或纯度: ≥98%

CAS编号: 209783-80-2
分子式: C₂₁H₂₀N₄O₃
分子量: 376.41
MDL号: MFCD03453552
PubChem编号: 4261

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货号 (SKU)	包装规格	是否现货	价格	数量
E125068-10mg	10mg	现货
E125068-50mg	50mg	现货
E125068-100mg	100mg	现货
E125068-250mg	250mg	现货

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histone deacetylase 1 Inhibitor histone deacetylase 2 Inhibitor histone deacetylase 3 Inhibitor histone deacetylase 9 Inhibitor

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基本描述

别名	恩替诺特
英文别名	SNDX-275\|SB16665\|D09338\|MLS006010183\|AC-8968\|CS-0511\|MS-275, A HDAC1 and HDAC3 inhibitor\|NSC756642\|NSC-756642\|DB11841\|Carbamic acid, 3-pyridinylmethyl ester\|MS-275,Entinostat, SNDX-275, MS-27-275\|W-201831\|N-[[4-[[(2-Aminophenyl)amino]carbonyl]phenyl]methy
规格或纯度	≥98%
英文名称	Entinostat (MS-275)
生化机理	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 sμggest that MS-275 may be particularly useful as an antineoplastic agent when combined with other drμgs, like adriamycin, inhibitors of poly (ADP-ribose) polymerase (PARP), or inhibitors of heat shock protein 90 (Hsp90).Benzamide derivative that inhibits histone deacetylase 1 (HDAC1) and HDAC2. Not active against HDAC4, 6, 8 and 10 (IC 50 >100μM). Exhibits anticancer chemotherapeutic, anti-metastatic, and neuroprotective properties.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。有毒，请参阅SDS以获取更多信息。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	Entinostat (MS-275)对HDAC1和HDAC3抑制作用强于与HDACs 4， 6， 8，和10，IC50分别为0.51 μM和1.7 μM。An HDAC inhibitor shown to inhibit angiogenesis and metastasis. Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10 An HDAC inhibitor shown to inhibit angiogenesis and metastasis.

产品属性

ALogP	2

名称和标识符

IUPAC Name	pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
INCHI	InChI=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)
InChi Key	INVTYAOGFAGBOE-UHFFFAOYSA-N
Canonical SMILES	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3
Isomeric SMILES	C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3
WGK Germany	3
PubChem CID	4261
分子量	376.41

数据库链接

PubChem CID	4261
CAS Registry No.	209783-80-2
ChEMBL Ligand	CHEMBL27759
Wikipedia	Entinostat

化学和物理性质

溶解性	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.
敏感性	对空气敏感，对热敏感
熔点	160 °C

安全和危险性（GHS）

象形图	Toxic Health Hazard Harmful
信号词	Danger
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation H335: May cause respiratory irritation H301: Toxic if swallowed H360: May damage fertility or the unborn child
预防措施声明	P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P270,P304+P340,P403+P233,P362+P364,P330,P203,P264+P265,P301+P316,P318,P337+P317,P332+P317,P319
WGK Germany	3

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参考文献

1. Hu E, Dul E, Sung CM, Chen Z, Kirkpatrick R, Zhang GF, Johanson K, Liu R, Lago A, Hofmann G et al.. (2003) Identification of novel isoform-selective inhibitors within class I histone deacetylases.. J Pharmacol Exp Ther, 307 (2): (720-8). [PMID:12975486]
2. Lin HS, Hu CY, Chan HY, Liew YY, Huang HP, Lepescheux L, Bastianelli E, Baron R, Rawadi G, Clément-Lacroix P. (2007) Anti-rheumatic activities of histone deacetylase (HDAC) inhibitors in vivo in collagen-induced arthritis in rodents.. Br J Pharmacol, 150 (7): (862-72). [PMID:17325656]
3. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. (2010) Chemical phylogenetics of histone deacetylases.. Nat Chem Biol, 6 (3): (238-243). [PMID:20139990]
4. Zhang ZY, Zhang Z, Schluesener HJ. (2010) MS-275, an histone deacetylase inhibitor, reduces the inflammatory reaction in rat experimental autoimmune neuritis.. Neuroscience, 169 (1): (370-7). [PMID:20451583]
5. Zhang ZY, Schluesener HJ. (2012) HDAC inhibitor MS-275 attenuates the inflammatory reaction in rat experimental autoimmune prostatitis.. Prostate, 72 (1): (90-9). [PMID:21538420]
6. Cantley MD, Bartold PM, Marino V, Fairlie DP, Le GT, Lucke AJ, Haynes DR. (2011) Histone deacetylase inhibitors and periodontal bone loss.. J Periodont Res, 46 (6): (697-703). [PMID:21745207]
7. Dear AE. (2016) Epigenetic Modulators and the New Immunotherapies.. N Engl J Med, 374 (7): (684-6). [PMID:26886527]

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