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[CAS NO. 522629-08-9] CGP 57380
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-10520 |
| Brand: | MCE |
| CAS: | 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 |
5 Publications Citing Use of MCE
Summary
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
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)
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 |
-
1.
-
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
References
- [1] Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11.
- [2] Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6
- [3] Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40.
- [4] Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307
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