SBI-0640756 (Synonyms: SBI-756) |
| Catalog No.GC19451 |
SBI-0640756 (SBI-756) est un inhibiteur de eIF4G1 et perturbe le complexe eIF4F.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1821280-29-8
Sample solution is provided at 25 µL, 10mM.
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SBI-0640756 is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.
SBI-0640756 is a water soluble inhibitor of eIF4G1. SBI-0640756 (0-1 μM) disrupts eIF4F complex in parent and BRAFi-resistant melanoma. SBI-0640756 shows inhibitory effect on human melanoma lines, and also suppresses AKT, NF-κB and AKT/mTORC1 activity[1].
SBI-0640756 (0.5 mg/kg, i.p.) delays tumor onset and reduces tumor incidence by 50% in NrasQ61K/Ink4a-/- genetic model. SBI-0640756 (1 mg/kg, 2 times per week, i.p.) in combination with BRAF inhibitor potently suppresses growth of established tumors and does not resume tumor growth in immunodeficient mice bearing A375 tumors[1].
[1]. Feng Y et al. SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex. Cancer Res, 2015 Dec 15, 75(24):5211-8.
Cell experiment: | WM793, Lu1205, WM1346 and WM1366 melanoma cells are seeded at 1500 cells in 50 μL per well in 384-well plates. Cells are allowed to attach overnight. SBI-0640756 (SBI-756) or derivatives analogs are serially diluted 2-fold with media from stock solutions and added to cells. Tests are performed in triplicate, and each microplate included media and DMSO control wells. Cell viability is assessed using ATPlite after 48 or 72 h. Cell growth inhibition is calculated as a percentage of DMSO-treated controls and plotted against the log drug concentration. IC50 values are interpolated from the resulting linear regression curve fit[1]. |
Animal experiment: | Mice[1]Six-week-old female nu/nu mice are allowed to acclimatize for 1 week. A375 cells (1 × 106, suspended in 200 μL 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) combination experiments, mice are either fed PLX4720-containing chow alone (AIN76A Roden Diet with 417 mg PLX4720/kg) for the control group or PLX4720-containing chow plus an IP injection of 1 mg/kg SBI-0640756 twice a week. For MEKi plus SBI-0640756 (SBI-756) experiments, PD0325901 at 20 mg/kg (formulated in 0.5% hydroxypropyl methylcellulose 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 twice a week (Tuesday and Friday)[1]. |
References: [1]. Feng Y et al. SBI-0640756 Attenuates the Growth of Clinically Unresponsive Melanomas by Disrupting the eIF4F Translation Initiation Complex. Cancer Res, 2015 Dec 15, 75(24):5211-8. | |
| Cas No. | 1821280-29-8 | SDF | |
| Synonymes | SBI-756 | ||
| Canonical SMILES | O=C1C(C(/C=C/C2=CC(F)=CN=C2)=O)=C(C3=CC=CC=C3)C4=C(C=CC(Cl)=C4)N1 | ||
| Formula | C23H14ClFN2O2 | M.Wt | 404.82 |
| Solubility | DMSO : ≥ 26 mg/mL (64.23 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4702 mL | 12.3512 mL | 24.7023 mL |
| 5 mM | 494 μL | 2.4702 mL | 4.9405 mL |
| 10 mM | 247 μL | 1.2351 mL | 2.4702 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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