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AES-135

COA COA
    级别和纯度:
  • ≥98%
有货

库存信息

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库存信息

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库存信息

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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
A649085-1mg
 1mg 期货 Stock Image
A649085-5mg
 5mg 期货 Stock Image
A649085-10mg
 10mg 期货 Stock Image
A649085-25mg
 25mg 期货 Stock Image
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Cell Cycle (7376) Cell Cycle/DNA Damage (2603) HDAC (161) Histone Modification (3105) 表观遗传学 (1497)
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基本描述

规格或纯度 ≥98%
英文名称 AES-135
生化机理 AES-135 是一种基于羟肟酸的泛 HDAC 抑制剂，可延长胰腺癌小鼠模型的生存期。AES-135 可抑制 HDAC3、HDAC6、HDAC8 和 HDAC11，其 IC 50 s 为 190-1100 nM。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
产品介绍


AES-135, a hydroxamic acid-based pan- HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer . AES-135 inhibits HDAC3 , HDAC6 , HDAC8 , and HDAC11 with IC 50 s ranging from 190-1100 nM

In Vitro

AES-135 inhibits cancer cells growth with IC 50 values of 2.3 µM, 1.4 µM, 0.27 µM, 0.94 µM, 1.9 µM, 2.72 µM, 2.1 µM, 15.0 µM, 1.6 µM and 19.2 µM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells . NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching C max 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57Bl/6 mice injected with KPC2 cells Dosage: 50 mg/kg Administration: Intraperitoneal injection; 5 days a week; for 1 month Result: Significantly increased survival of mice.

Form:Solid

IC50& Target:HDAC6 190 nM (IC 50 ) HDAC11 636 nM (IC 50 ) HDAC3 654 nM (IC 50 ) HDAC8 1100 nM (IC 50 )
纯度 ≥98%

关联靶点（人）

HDAC6 Tclin 组蛋白去乙酰化酶6(Histone deacetylase 6) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC11 Tclin 组蛋白去乙酰化酶11(Histone deacetylase 11) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC3 Tclin 组蛋白去乙酰化酶3(Histone deacetylase 3) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
HDAC8 Tclin Histone deacetylase 8 (4516 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC10 Tclin Histone deacetylase 10 (801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC3 Tclin Histone deacetylase 3 (3654 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC4 Tclin Histone deacetylase 4 (2328 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STAT3 Tchem Signal transducer and activator of transcription 3 (3313 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HDAC11 Tclin Histone deacetylase 11 (967 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
K562 (73714 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-468 (9477 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PC-3 (62116 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MDA-MB-231 (73002 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MV4-11 (7307 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Panc1005 (135 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
STAT5B Tchem Signal transducer and activator of transcription 5B (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MOLM-13 (2241 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Hdac1 Histone deacetylase 1 (93 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 未知
IIUPAC Name 4-[(4-tert-butylphenyl)methyl-[2-[(4-fluorophenyl)sulfonyl-[(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxybenzamide
INCHI 1S/C33H29F6N3O5S/c1-33(2,3)21-8-4-19(5-9-21)16-42(23-12-6-20(7-13-23)32(44)40-45)26(43)18-41(48(46,47)24-14-10-22(34)11-15-24)17-25-27(35)29(37)31(39)30(38)28(25)36/h4-15,45H,16-18H2,1-3H3,(H,40,44)
InChi Key LTRKEOBJRDKIHB-UHFFFAOYSA-N
Smiles CC(C)(C)C1=CC=C(C=C1)CN(C2=CC=C(C=C2)C(=O)NO)C(=O)CN(CC3=C(C(=C(C(=C3F)F)F)F)F)S(=O)(=O)C4=CC=C(C=C4)F
Isomeric SMILES CC(C)(C)C1=CC=C(C=C1)CN(C2=CC=C(C=C2)C(=O)NO)C(=O)CN(CC3=C(C(=C(C(=C3F)F)F)F)F)S(=O)(=O)C4=CC=C(C=C4)F
PubChem CID 137628685
MeSH Entry Terms 4-((4-tert-butylphenyl)methyl-(2-((4-fluorophenyl)sulfonyl-((2,3,4,5,6-pentafluorophenyl)methyl)amino)acetyl)amino)-N-hydroxybenzamide;AES-135
分子量 693.66

化学和物理性质

溶解性 DMSO : 100 mg/mL (144.16 mM; Need ultrasonic)

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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