2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway GPCR/G Protein
  3. EGFR Ras
  4. SOS1/EGFR-IN-1

SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM).

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SOS1/EGFR-IN-1 Chemical Structure

SOS1/EGFR-IN-1 Chemical Structure

CAS No. : 2956724-20-0

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Based on 1 publication(s) in Google Scholar

SOS1/EGFR-IN-1 Related Antibodies

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Description

SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM)[1].

In Vitro

SOS1/EGFR-IN-1 (0.5, 12.5 μM; 15 min) inhibits the proliferation of PC-3 cells and has a stronger inhibitory effect on SOS1 and EGFR activity than either SOS1 or EGFR inhibitors alone or a combination of both[1].
SOS1/EGFR-IN-1 (0.5, 2.5, 12.5 μM; 15 days) can cause cell apoptosis and cell cycle arrest to exert potent antiproliferative activity in PC-3 cells[1].
SOS1/EGFR-IN-1 (0.5, 12.5 μM; 15 min) reduces RAS-GTP levels and blocks EGF-mediated up-regulation of pAKT levels in cell line PC-3[1].
SOS1/EGFR-IN-1 (0.5, 2.5, 12.5 μM; 48 h) decreases the number of HUVECs migrating to the scratched area relative to the control group and the migration indexes dropped significantly with increasing concentrations of SE-9[1].

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

SOS1/EGFR-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: Prostate cancer cell line PC-3
Concentration: 0.5, 2.5, 12.5 μM
Incubation Time: 15 day
Result: Resulted in a concentration-dependent decrease in cyclin D1 and CDK4 expression.

Cell Viability Assay[1]

Cell Line: DLD-1, K562, HepG2, A549, PC-3 and RWPE-1 cells
Concentration:
Incubation Time: 72 h
Result: Had better cytotoxicity of PC-3 cells (IC50 = 0.45±0.03 μM) compared to KRAS mutation-driven cancer cells (IC50= 0.55 ~ 0.81 μM).

Western Blot Analysis[1]

Cell Line: Prostate cancer cell line PC-3
Concentration: 0.5, 12.5 μM
Incubation Time: 15 min
Result: Blocked significantly EGF-mediated upregulation of pAKT levels.
Reduced RAS-GTP levels and the corresponding pAKT and pERK levels.
Attenuated EGF-induced upregulation of pEGFR and pAKT levels

Cell Cycle Analysis[1]

Cell Line: Prostate cancer cell line PC-3
Concentration: 0.5, 2.5, 12.5 μM
Incubation Time: 15 day
Result: Enhanced remarkably cell distribution in the G1 phase in a dose-dependent manner and Reduced S and G2 phase distribution.
In Vivo

SOS1/EGFR-IN-1 (5, 20 mg/kg, ip; every 4 days for a total of six times) could exert effective apoptosis-inducing and angiogenesis- and proliferation-reducing activities. SOS1/EGFR-IN-1 possesses strong in vivo antitumor activity without obvious adverse side effects in PC-3 cell-derived prostate cancer xenograft model[1].
Pharmacokinetic Analysis inPC-3 cell-derived prostate cancer xenograft mode[1]

Compound name Route Dose (mg/kg) T1/2 (h) Cmax (μg/mL) Tmax (h) AUC (ng/h/mL)
AXE p.o. 10 1.74 637 4.13 7502
SE-9 p.o. 10 2.81 865 3.94 8530

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

Animal Model: Six-week-old female BALB/c nude mice[1]
Dosage: 5, 20 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increased significantly TUNEL staining and decreased obviously the staining of CD31 and Ki67.
Molecular Weight

397.44

Formula

C22H24FN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC([C@@H](C)NC2=C3C=C(OC4CCOCC4)C(OC)=CC3=NC=N2)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (251.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5161 mL 12.5805 mL 25.1610 mL
5 mM 0.5032 mL 2.5161 mL 5.0322 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (12.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (12.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5161 mL 12.5805 mL 25.1610 mL 62.9026 mL
5 mM 0.5032 mL 2.5161 mL 5.0322 mL 12.5805 mL
10 mM 0.2516 mL 1.2581 mL 2.5161 mL 6.2903 mL
15 mM 0.1677 mL 0.8387 mL 1.6774 mL 4.1935 mL
20 mM 0.1258 mL 0.6290 mL 1.2581 mL 3.1451 mL
25 mM 0.1006 mL 0.5032 mL 1.0064 mL 2.5161 mL
30 mM 0.0839 mL 0.4194 mL 0.8387 mL 2.0968 mL
40 mM 0.0629 mL 0.3145 mL 0.6290 mL 1.5726 mL
50 mM 0.0503 mL 0.2516 mL 0.5032 mL 1.2581 mL
60 mM 0.0419 mL 0.2097 mL 0.4194 mL 1.0484 mL
80 mM 0.0315 mL 0.1573 mL 0.3145 mL 0.7863 mL
100 mM 0.0252 mL 0.1258 mL 0.2516 mL 0.6290 mL
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SOS1/EGFR-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SOS1/EGFR-IN-12956724-20-0EGFRRasEpidermal growth factor receptorErbB-1HER1Multitarget medicationsSOS1/EGFR inhibitorPC-3BALB/c miceInhibitorinhibitorinhibit

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