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CGP 57380

CGP 57380 (MNK1 Inhibitor) 是细胞渗透的吡唑-嘧啶类化合物，是一种具有选择性的Mnk1抑制剂，IC50值为 2.2 μM。

CAS号

522629-08-9

分子式

C11H9FN6

主要靶点

MNK|Apoptosis

仅限科研使用

Cat No : CM05195

Print datasheet

Synonyms

N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺|MNK1 Inhibitor

验证数据展示

  • CAS No.: 522629-08-9

    CGP 57380
    CAS#: 522629-08-9

产品信息

CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.

CAS号 522629-08-9
分子式 C11H9FN6
主要靶点 MNK|Apoptosis
主要通路 MAPK信号通路|凋亡
分子量 244.23
纯度 99.89%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺|MNK1 Inhibitor

靶点活性

MNK1:2.2 μM

体内活性

CGP57380 (40 mg/kg/d i.p.) potently abrogates the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs. [4]

体外活性

CGP57380 inhibits phosphorylation of eIF4E in vitro with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. [1] CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. [2] CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). [3] CGP57380 prevents the serial replating function of BC progenitors. [4]

溶解度

DMSO:45 mg/mL (184.3 mM),Ethanol:<1 mg/mL,H2O:<1 mg/mL

参考文献

1.Knauf U, et al. Mol Cell Biol. 2001, (16), 5500-5511.
2.Ishida M, et al. Circ Res. 2003, 93(12), 1218-1224.
3.Chrestensen CA, et al. Genes Cells. 2007, 12(10), 1133-1140.
4.Lim S, et al. Proc Natl Acad Sci U S A. 2013, 110(25), E2298-E2307.

The molarity calculator equation

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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