SBI-0640756-SBI-756-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESBI-0640756Cat. No.: HY-19560CAS No.: 1821280-29-8Synonyms: SBI-756分式: CHClFNO分量: 404.82作靶点: Eukaryotic Initiation Factor (eIF)作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据

2、体外实验 DMSO : 26 mg/mL (64.23 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4702 mL 12.3512 mL 24.7023 mL5 mM 0.4940 mL 2.4702 mL 4.9405 mL10 mM 0.2470 mL 1.2351 mL 2.4702 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 SBI-0640756

3、 (SBI-756)种溶于的 eIF4G1 抑制剂，能够破坏 eIF4F 复合体。IC50 & Target eIF4G1 1体外研究SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1. SBI-0640756 (SBI-756) (0-1 M) disrupts1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEeIF4F complex in parent and BRAFi-resistant melanoma. SBI-0640756 (SBI-756) shows in

4、hibitory effect onhuman melanoma lines, and also suppresses AKT, NF-B and AKT/mTORC1 activity 1.体内研究 SBI-0640756 (SBI-756) (0.5 mg/kg, i.p.) delays tumor onset and reduces tumor incidence by 50% inNrasQ61K/Ink4a/ genetic model. SBI-0640756 (SBI-756) (1 mg/kg, 2 times per week, i.p.) in combinationwi

5、th BRAF inhibitor potently suppresses growth of established tumors and does not resume tumor growth inimmunodeficient mice bearing A375 tumors 1.PROTOCOLCell Assay 1 WM793, Lu1205, WM1346 and WM1366 melanoma cells are seeded at 1500 cells in 50 L per well in 384-well plates. Cells are allowed to att

6、ach overnight. SBI-0640756 (SBI-756) or derivatives analogs are seriallydiluted 2-fold with media from stock solutions and added to cells. Tests are performed in triplicate, and eachmicroplate included media and DMSO control wells. Cell viability is assessed using ATPlite after 48 or 72 h.Cell growt

7、h inhibition is calculated as a percentage of DMSO-treated controls and plotted against the logdrug concentration. IC50 values are interpolated from the resulting linear regression curve fit 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice

8、1Administration 1 Six-week-old female nu/nu mice are allowed to acclimatize for 1 week. A375 cells (1 106, suspended in200 L sterile PBS) are injected into subcutaneous flank tissue. When the xenograft size reach -250 mm3,mice are sorted into different groups. For PLX4720 and SBI-0640756 (SBI-756) c

9、ombination experiments,mice are either fed PLX4720-containing chow alone (AIN76A Roden Diet with 417 mg PLX4720/kg) for thecontrol group or PLX4720-containing chow plus an IP injection of 1 mg/kg SBI-0640756 twice a week. ForMEKi plus SBI-0640756 (SBI-756) experiments, PD0325901 at 20 mg/kg (formula

10、ted in 0.5% hydroxypropylmethylcellulose plus 0.2% Tween-80) is administered by oral gavage twice a week (Monday and Thursday)for the control group, or PD035901 plus IP injection of 1 mg/kg SBI-0640756 (SBI-756) is administered twicea week (Tuesday and Friday) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Feng Y et al. SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation InitiationComplex. Cancer Res, 2015 Dec 15, 75(24):5211-8.McePdfHeightCaution: Product has not be