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

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.
Unlabeled CAS

SMILES

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

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SOS1/EGFR-IN-1
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HY-158310
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