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S116836

CAS No. : 1257628-57-1

MCE 国际站：S116836

产品活性：S116836 是一种有效的，具有口服活性的 BCR-ABL 酪氨酸激酶抑制剂 (TKI)，可阻断野生型和 T315I BCR-ABL。S116836 将 BaF3/WT 和 BaF3/T315I 细胞阻滞在细胞周期的 G0/G1 期，诱导凋亡 (apoptosis)，增加 ROS 的产生，减少 GSH 的产生。S116836 还抑制 SRC、LYN、HCK、LCK 和 BLK，以及受体酪氨酸激酶，如 FLT3、TIE2、KIT、PDGFR-β。具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：Bcr-Abl  |  Apoptosis  |  PDGFR

In Vitro: S116836 (0.01-1 μM; 24 hours) significantly reduces the cellular proliferation of BaF3/WT and BaF3/T315I cells (IC₅₀ values of 0.05 μM and 0.20 μM, respectively).
S116836 (0.01-1 μM; 24 hours) significantly downregulates the expression level of p-BCR-ABL in BaF3/WT cells. S116836 (0.01-1 μM; 24 hours) also significantly downregulates the expression level of p-Crkl and p-STAT5 (downstream signaling proteins of BCR-ABL) in both BaF3/WT and BaF3/T315I cells.
S116836 (0.1, 0.3, and 0.5 μM; 24 hours) arrests the BaF3/WT and BaF3/T315I cells in G0/G1 phase of the cell cycle.
S116836 (0.3 and 0.5 μM; 24 hours) increases ROS production and decreases GSH levels in BaF3/WT and BaF3/T315I cells.
S116836 (0.1, 0.3, and 0.5 μM; 24 hours) induces apoptosis in BaF3/WT and BaF3/T315I cells.
S116836 potently inhibits PDGFRα and its downstream signaling molecules such as STAT3, AKT, and Erk1/2. S116836 effectively inhibits the growth of the WT and T674I FIP1L1-PDGFRα-expressing neoplastic cells.

In Vivo: S116836 (100 or 200 mg/kg; i.p.; q3d×6, athymic NCR nude mice) decreases the volume and weight of xenograft tumors expressing WT and T315I mutant BCR-ABL.
S116836 (200mg/kg/d, oral gavage for 14 days) inhibits the growth of xenografted T674I-FIP1L1-PDGFRα cells in nude mice.

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