2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. Nanatinostat TFA

Nanatinostat TFA  (Synonyms: CHR-3996 TFA)

目录号: HY-13432A
产品使用指南 技术支持

Nanatinostat (CHR-3996) TFA 是一种强效、I 类选择性、具有口服活性的 HDAC 抑制剂，对 HDAC1、HDAC2 和 HDAC3 的 IC50 分别为 3 nM、4 nM 和 7 nM。Nanatinostat TFA 对 HDAC5 (IC50 为 200 nM) 和 HDAC6 (IC50 为 2100 nM) 的活性较低。Nanatinostat TFA 可诱导骨髓瘤细胞凋亡 (apoptosis)。Nanatinostat TFA 具有强效的抗癌作用，例如针对骨髓瘤、晚期实体瘤和结直肠癌。

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Nanatinostat TFA

Nanatinostat TFA Chemical Structure

CAS No. : 1256448-48-2

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Nanatinostat TFA 的其他形式现货产品:

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Nanatinostat TFA 相关抗体

Top Publications Citing Use of Products

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer[1][2][3].

IC50 & Target[1]

HDAC1

3 nM (IC50)

HDAC2

4 nM (IC50)

HDAC3

7 nM (IC50)

HDAC

8 nM (IC50)

HDAC5

200 nM (IC50)

HDAC6

2100 nM (IC50)

体外研究
(In Vitro)

Nanatinostat (CHR-3996) (0.0001-1 μM; 48 小时) TFA 在骨髓瘤细胞系中抑制细胞增殖，不同细胞系的 LC50 值在 30.3-97.6 nM 之间[2]。
Nanatinostat (250-100 nM；8-48 小时) TFA 在 H929 和 RPMI-8226 骨髓瘤细胞系中诱导细胞凋亡，并增加乙酰化 H3K9 水平[2]。
Nanatinostat (0-200 nM；24 小时) TFA 在骨髓基质细胞与骨髓瘤细胞共培养体系中，降低骨髓基质细胞分泌的 IL-6 和 VEGF 水平[2]。
Nanatinostat (250 nM 和 100 nM；48 小时) TFA 在 H929 和 RPMI-8226 骨髓瘤细胞系中使细胞周期阻滞在 G0/G1 期[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Nanatinostat TFA 相关抗体:

Cell Viability Assay[2]

Cell Line: H929, RPMI-8226, KMS11, LP-1, MM1-S cells
Concentration: 0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 48 hours
Result: The cell viability decreased.

Apoptosis Analysis[2]

Cell Line: H929 and RPMI-8226 myeloma cell lines
Concentration: 100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time: 8 hours, 24 hours, 48 hours
Result: The percentage of apoptotic cells increased, with an increase in both early and late apoptotic cells.

Cell Cycle Analysis[2]

Cell Line: H929 and RPMI-8226 myeloma cell lines
Concentration: 100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time: 48 hours
Result: The cell cycle was arrested at the G0/G1 phase.

Western Blot Analysis[2]

Cell Line: H929 and RPMI-8226 myeloma cell lines
Concentration: 100 nM (RPMI-8226 cells), 250 nM (H929 cells)
Incubation Time: 8 hours, 24 hours, 48 hours
Result: The pro-apoptotic DNase Endonuclease G and p53 downstream mediator Noxa were up-regulated, and caspase 9 was cleaved.
体内研究
(In Vivo)

Nanatinostat (CHR-3996) (50 mg/kg；口服；每日一次；14 天) TFA 在雌性 CrTac:NCr-Fox1 ν 小鼠 HCT116 肿瘤异种移植模型中几乎完全抑制肿瘤生长[1]。
Nanatinostat (25-50 mg/kg；口服；每日一次；19 天) TFA 在雌性 BALB/c 裸鼠 LoVo 人结肠异种移植模型中，可显著减小肿瘤体积且呈剂量依赖性[1]。
Nanatinostat (30 mg/kg；口服；每日一次；连续 28 天) TFA 在 NOD/SCID IL2R gammanull 小鼠骨髓瘤模型中可有效抑制肿瘤生长[2] 。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CrTac:NCr-Fox1(nu) mice (6-8 weeks old; inoculated bilaterally sc with 2 million human HCT116 colon carcinoma cells)[1].
Dosage: 50 mg/kg
Administration: Orally administered, once daily, for 14 days
Result: Almost completely suppressed tumor growth, and the tumor concentration was high, with a tumor-to-plasma concentration ratio reflecting good distribution to the tumor.
Animal Model: Female BALB/c nude mice (inoculated with LoVo human colorectal xenograft)[1].
Dosage: 25 mg/kg and 50 mg/kg
Administration: Orally administered, once daily, for 19 days
Result: Significantly reduced tumor volume, and the effect was dose-dependent.
Animal Model: NOD/SCID IL2R gammanull mice (inoculated subcutaneously with  2×106 H929 myeloma cells)[2].
Dosage: 30 mg/kg
Administration: Orally administered, once daily, for up to 28 days
Result: Effectively inhibited tumor growth.
Clinical Trial
分子量

508.43

Formula

C22H20F4N6O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Nanatinostat TFA 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nanatinostat1256448-48-2CHR-3996CHR3996CHR 3996HDACApoptosisHistone deacetylasesHDAC1HDAC2HDAC3apoptosis myelomaadvanced solid tumours and colorectal cancerInhibitorinhibitorinhibit

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