Cat. No.: HY-158310

SOS1/EGFR-IN-1

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Based on 1 Customer Validation

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).

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

Purity: 99.54%
CAS No.: 2956724-20-0
Formula: C₂₂H₂₄FN₃O₃
Molecular Weight:397.44

Storage:

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

SOS1/EGFR-IN-1 Chemical Structure

CAS No.: 2956724-20-0

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

All Ras Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-427	IC₅₀	0.55 μM Compound: SE-9	Antiproliferative activity against human A-427 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A-427 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
Calu-1	IC₅₀	0.55 μM Compound: SE-9	Antiproliferative activity against human Calu-1 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human Calu-1 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
NCI-H358	IC₅₀	0.55 μM Compound: SE-9	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
PC-3	IC₅₀	>10 μM Compound: SE-9	Antiproliferative activity against human PC-3 cells transfected with SOS1 and EGFR shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells transfected with SOS1 and EGFR shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
PC-3	IC₅₀	0.43 μM Compound: SE-9	Antiproliferative activity against human PC-3 cells transfected with control shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells transfected with control shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
PC-3	IC₅₀	0.45 μM Compound: SE-9	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
PC-3	IC₅₀	3.92 μM Compound: SE-9	Antiproliferative activity against human PC-3 cells transfected with SOS1 shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells transfected with SOS1 shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
PC-3	IC₅₀	5.48 μM Compound: SE-9	Antiproliferative activity against human PC-3 cells transfected with EGFR shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells transfected with EGFR shRNA assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
RWPE-1	IC₅₀	>10 μM Compound: SE-9	Antiproliferative activity against human RWPE-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human RWPE-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]
SK-LU-1	IC₅₀	0.55 μM Compound: SE-9	Antiproliferative activity against human SK-LU-1 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-LU-1 cells harboring KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 38630077]

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.

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)	T_1/2 (h)	C_max (μg/mL)	T_max (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.

Chemical Information

CAS No. 2956724-20-0
Appearance Solid
Molecular Weight 397.44
Formula C₂₂H₂₄FN₃O₃
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5161 mL

12.5805 mL

25.1610 mL

5 mM

0.5032 mL

2.5161 mL

5.0322 mL

10 mM

0.2516 mL

1.2581 mL

2.5161 mL

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.

Molarity Calculator

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

Mass Mass

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zheng L, et al. Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer[J]. Journal of Medicinal Chemistry, 2024. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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All EGFR Isoforms

All Ras Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

SOS1/EGFR-IN-1 Related Classifications

HY-158310 Related Classifications