1. MAPK/ERK Pathway
    Apoptosis
  2. MNK
    Apoptosis
  3. CGP 57380

CGP 57380 

Cat. No.: HY-10520 Purity: 98.03%
Handling Instructions

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

For research use only. We do not sell to patients.

CGP 57380 Chemical Structure

CGP 57380 Chemical Structure

CAS No. : 522629-08-9

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10 mM * 1  mL in DMSO USD 196 In-stock
Estimated Time of Arrival: December 31
10 mg USD 178 In-stock
Estimated Time of Arrival: December 31
50 mg USD 734 In-stock
Estimated Time of Arrival: December 31
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Description

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

IC50 & Target[1]

MNK1

2.2 μM (IC50)

In Vitro

CGP57380 inhibits phosphorylation of eIF4E in cellular assays 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].

In Vivo

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

Molecular Weight

244.23

Formula

C₁₁H₉FN₆

CAS No.

522629-08-9

SMILES

NC1=NC=NC2=C1C(NC3=CC=C(F)C=C3)N=N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (24.57 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0945 mL 20.4725 mL 40.9450 mL
5 mM 0.8189 mL 4.0945 mL 8.1890 mL
10 mM 0.4095 mL 2.0473 mL 4.0945 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (10.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors.

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

Animal Administration
[4]

CD34+ cells (5×105) or GMPs (1×105) are resuspended in 25 μL 1% FBS/PBS solution and injected into the right femur of 8- to 10-wk-old sublethally irradiated (200 cGy) female mice (n=5 mice per group). Mice injected with 1% FBS/PBS solution serve as a sham control for each experiment. Beginning at 4 wk posttransplantation, mice are monitored for engraftment of human cells by flow cytometry. At 6 wk after transplantation, engrafted mice are treated with vehicle alone, dasatinib (5 mg/kg/d) by gavage, or CGP57380 (40 mg/kg/d) intraperitoneally for 3 wk (n=5 mice per group). At the end of treatment, mice are euthanized, and CD45+ cells are isolated from BM and spleen by using anti-human CD45-specific immunomagnetic microbeads. An aliquot of 1×105 human CD45+ cells is seeded into methylcellulose for the colony forming cell (CFC) assay, and colonies are enumerated after 2 wk. All of the remaining human cells from each primary transplant recipient are then transplanted by intrafemoral injection into secondary recipients, and human engraftment is monitored at 2-wk intervals beginning at 4 wk. At the end of 16 wk, all mice are euthanized. Engraftment in BM and blood is assessed by flow cytometry, and BCR-ABL1 transcripts are detected by RT-PCR.

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

References
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Keywords:

CGP 57380CGP57380CGP-57380MNKApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseInhibitorinhibitorinhibit

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CGP 57380
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HY-10520
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