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SOS1/EGFR-IN-1

CAS No. : 2956724-20-0

MCE 站：SOS1/EGFR-IN-1

产品活性：SOS1/EGFR-IN-1 (compound SE-9) 是一种针对前列腺癌的双重靶点抑制剂。SOS1/EGFR-IN-1 通过抑制 SOS1 和 EGFR，进而有效抑制了它们的下游效应分子。SOS1/EGFR-IN-1 诱导细胞凋亡 (apoptosis) 和 G1 期细胞周期阻滞，减少血管生成和迁移。SOS1/EGFR-IN-1 在前列腺癌细胞 PC-3 (IC₅₀=0.45±0.03 μM) 中表现出显著的抗肿瘤效果。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK  |  GPCR/G Protein  |  MAPK/ERK Pathway

作用靶点：EGFR  |  Ras

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.
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.
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.
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.

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.
Pharmacokinetic Analysis inPC-3 cell-derived prostate cancer xenograft mode

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