1. Cell Cycle/DNA Damage MAPK/ERK Pathway
  2. MNK Eukaryotic Initiation Factor (eIF)
  3. MNK1/2-IN-7

MNK1/2-IN-7 (compound 20j) 是一种口服有效的 MNK1/2 的抑制剂,具有抗癌活性和 hERG 安全性。MNK1/2-IN-7 还抑制 eIF4E 的磷酸化,抑制 MNK/eIF4E 信号通路和癌细胞增殖。MNK1/2-IN-7 与 Ibrutinib (HY-109970) 有协同作用。

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MNK1/2-IN-7 Chemical Structure

MNK1/2-IN-7 Chemical Structure

CAS No. : 2548283-27-6

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查看 MNK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970).[15][1].

IC50 & Target

MNK1

4.4 nM (IC50, [1])

MNK2

.4 nM (IC50, [1])

体外研究
(In Vitro)

MNK1/2-IN-7 (1.25-5 μM; 24 h) 抑制 Hela 细胞中 eIF4E 的磷酸化 (IC50=90.5 nM) 并下调 A549 细胞中 eIF4E 和 4E-BP1 的磷酸化[1]
MNK1/2-IN-7 在人、犬、大鼠的肝脏微粒中表现出稳定性,T1/2 分别为 62.6 min,>120 min,和 64.6 min[1]

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

Western Blot Analysis[1]

Cell Line: A549 cell line
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 24 h
Result: Downregulated the phosphorylation of eIF4E and 4E-BP1.
体内研究
(In Vivo)

MNK1/2-IN-7 (5 mg/kg; po; 单剂量) 在大鼠中表现出可接受的暴露和生物利用度,具有口服有效性[1]
MNK1/2-IN-7 (10 mg/kg; po; 17 d) 在 DOHH2 的异种异植小鼠模型中,有效使得肿瘤消退,且不影响小鼠体重。MNK1/2-IN-7 还与 Ibrutinib (HY-109970) 有协同作用[1]

在 SD 大鼠中的药代动力学分析[1]

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (μg/mL) AUC0-t (h·μg/mL) AUC0-∞ (h·μg/mL) Cl (mL/h/kg) F (%)
i.v. 1 13.8 0.083 1.3 10.0 14.4 70.2 /
p.o. 5 >24 6 1.5 23.3 NA / 46.86

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

Animal Model: GCB-DLBCL DOHH2 xenograft tumors model in mouse[1]
Dosage: 10 mg/kg
Administration: po; once daily for 17 days; or combination of 3 mg/kg Ibrutinib
Result: Resulted tumor regression
Achieved a greater TGI value of 54% for combination group at the end of treatment compared to the value for a single administration or ibrutinib administration.
分子量

505.61

Formula

C31H31N5O2

CAS 号
Unlabeled CAS

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
  • 摩尔计算器

  • 稀释计算器

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

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产品名称:
MNK1/2-IN-7
目录号:
HY-163479
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