1. Cell Cycle/DNA Damage
  2. Eukaryotic Initiation Factor (eIF)

SBI-0640756 (Synonyms: SBI-756)

Cat. No.: HY-19560 Purity: >98.0%
Handling Instructions

SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.

For research use only. We do not sell to patients.

SBI-0640756 Chemical Structure

SBI-0640756 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 192 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
25 mg USD 720 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.

IC50 & Target

eIF4G1[1]

In Vitro

SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1. SBI-0640756 (SBI-756) (0-1 μM) disrupts eIF4F complex in parent and BRAFi-resistant melanoma. SBI-0640756 (SBI-756) shows inhibitory effect on human melanoma lines, and also suppresses AKT, NF-κB and AKT/mTORC1 activity[1].

In Vivo

SBI-0640756 (SBI-756) (0.5 mg/kg, i.p.) delays tumor onset and reduces tumor incidence by 50% in NrasQ61K/Ink4a–/– genetic model. SBI-0640756 (SBI-756) (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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 26 mg/mL (64.23 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4702 mL 12.3512 mL 24.7023 mL
5 mM 0.4940 mL 2.4702 mL 4.9405 mL
10 mM 0.2470 mL 1.2351 mL 2.4702 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

404.82

Formula

C₂₃H₁₄ClFN₂O₂

SMILES

O=C1C(C(/C=C/C2=CC(F)=CN=C2)=O)=C(C3=CC=CC=C3)C4=C(C=CC(Cl)=C4)N1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Inquiry Information

Product Name:
SBI-0640756
Cat. No.:
HY-19560
Quantity:

SBI-0640756

Cat. No.: HY-19560