4EGI-1 化学構造
分子量: 451.28

高品質保証

Quality Control & MSDS

製品説明

製品の説明

生物活性

製品説明 4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 μM.
ターゲット eIF4E/eIF4G
IC50 25 μM (KD) [1]
In vitro試験 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. [1] 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. [2] In addition, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. [3]
In vivo試験
臨床試験
特集

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 Jurkat cells and A549 lung cancer cells.
濃度 ~60 μM
反応時間 24 hours
実験の流れ 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download 4EGI-1 SDF
分子量 451.28
化学式

C18H12Cl2N4O4S

CAS No. 315706-13-9
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 90 mg/mL (199.43 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 α-[2-[4-(3,4-Dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitro-benzenepropanoic acid

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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