| CAS NO: | 315706-13-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 451.28 |
|---|---|
| Formula | C18H12Cl2N4O4S |
| CAS No. | 315706-13-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 90 mg/mL (199.4 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name: alpha-[2-[4-(3,4-Dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitro-benzenepropanoic acid InChi Key: KFRKRECSIYXARE-HYARGMPZSA-N InChi Code: InChI=1S/C18H12Cl2N4O4S/c19-12-6-5-10(7-13(12)20)15-9-29-18(21-15)23-22-14(17(25)26)8-11-3-1-2-4-16(11)24(27)28/h1-7,9H,8H2,(H,21,23)(H,25,26)/b22-14+ SMILES Code: O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2 |
| Synonyms | 4EGI-1; 4-EGI1; 4 EGI 1; 4EGI1; 4EGI1; 4 EGI1; 4-EGI-1 |
| In Vitro | In vitro activity: 4EGI-1 disrupts the eIF4F complex and inhibits Cap-dependent translation in vitro. 4EGI-1 has proapoptotic activity in Jurkat cells, and potently inhibits cell growth with IC50 of approximately 6 μM in A549 lung cancer cells. 4EGI-1 augments TRAIL-induced apoptosis through induction of DR5 and down-regulation of c-FLIP, independent of inhibition of cap-dependent protein translation in human lung cancer cells. In addition, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. Kinase Assay: As a mimic peptide of 4E-BP, 4EGI-1 competes with eIF4G and disrupts the association of eIF4E/eIF4G. The KD value for 4EGI-1 binding to eIF4E is 25μM. 4EGI-1 can not affect the binding of 4E-BP to eIF4E and instead causes increase of this binding level. In addition, 4EGI-1 is found to inhibit the Cap-dependent translation while enhances the initiation factor-independent translation. In Jurkat leukemia T cells, 4EGI-1 also causes eIF4G to be displaced from eIF4E. Cell Assay: Cell viability is measured by treatment of Jurkat cells with compound for 24 h and by determination of intracellular ATP using the CellTiterGlo assay. For measurement of apoptotic DNA fragmentation, cells are treated for 24 h with 60 μM EGI-1 or 6.65 μM camptothecin in the presence or absence of 100 mM zVAD-FMK, a broad-spectrum caspase inhibitor. After fixation and staining with PI, cellular DNA content is determined by FACS analysis in a FACS Calibur machine. Nuclear morphology after 24 h EG1-1 treatment is visualized by staining of cells with Hoechst dye and fluorescence microscopy. For the A549 lung cancer cells, cell growth in the presence of 4EGI-1 is determined using the SRB staining method. |
|---|---|
| In Vivo | 4EGI-1 (75 mg/kg, i.p.) inhibits breast cancer stem cells (CSC) tumor growth and tumorangiogenesis in vivo. 4EGI-1 (75 mg/kg, i.p.) shows inhibitory effect on the tumor volume and weight in mice bearing U87 cells |
| Animal model | Mice: In the tumor xenografted assay, 1×105 breast cancer stem cells (CSCs) are mixed with 100 μL Matrigel/DMEM mixture (Matrigel: DMEM = 1:2). Breast CSCs/Matrigel/DMEM mixtures are injected into NOD/SCID female mice mammary glands by subcutaneous injection. After the tumor formation (about 75 mm3 in volume, 5 mice/group), DMSO, or 75 mg/kg [E]-4EGI-1, or 75 mg/kg [Z]-4EGI-1 is injected into the mice by intraperitoneal injection daily for 30 days. Tumor volumes are measured every three days. At the 30th day, mice are sacrificed and tumors are excised. Tumors weights are measured. Tumor tissue samples are used for immunohistostaining, Western blot and immunoprecipitation analyses. |
| Formulation & Dosage | 75 mg/kg; i.p. |
| References | Cell. 2007 Jan 26;128(2):257-67; Neoplasia. 2010 Apr;12(4):346-56; Clin Cancer Res. 2013 Jun 15;19(12):3212-23. |
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