[CAS NO. 522629-08-9] CGP 57380

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PRODUCTS SPECIFICATIONS [522629-08-9]

Catalog

HY-10520

Brand

MCE

CAS

522629-08-9

DESCRIPTION [522629-08-9]

Overview

MDL	MFCD03861062
Molecular Weight	244.23
Molecular Formula	C11H9FN6
SMILES	NC1=NC=NC2=C1C(NC3=CC=C(F)C=C3)N=N2

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

5 Publications Citing Use of MCE

Summary

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC ₅₀ of 2.2 μM, but has no inhibitory activity against p38, JNK1 , ERK1/2, PKC , or Src-like kinases.

IC50 & Target

MNK1

2.2 μM (IC ₅₀ )

In Vitro

CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC ₅₀ 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] .

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

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] .

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

Appearance

Solid

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)

H ₂ O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

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 available by MCE.