[CAS NO. 522629-08-9]  CGP 57380

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PRODUCTS SPECIFICATIONS [522629-08-9]

Store
Catalog
SLK-S7421
Brand
Selleck
CAS
522629-08-9

DESCRIPTION [522629-08-9]

Overview

MDLMFCD03861062
Molecular Weight244.23
Molecular FormulaC11H9FN6
SMILESNC1=C2C(NN=C2NC3=CC=C(F)C=C3)=NC=N1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM4.0945 mL20.4725 mL40.9450 mL
5 mM0.8189 mL4.0945 mL8.1890 mL
10 mM0.4095 mL2.0473 mL4.0945 mL
50 mM0.0819 mL0.4095 mL0.8189 mL

Description

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

Targets

MNK1 [1]
(Cell-free assay)
2.2 μM

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. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). CGP57380 prevents the serial replating function of BC progenitors.

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.