| Bioactivity | S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies[1][2][3]. |
| Invitro | 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)[1].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[1].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[1].S116836 (0.3 and 0.5 μM; 24 hours) increases ROS production and decreases GSH levels in BaF3/WT and BaF3/T315I cells[1].S116836 (0.1, 0.3, and 0.5 μM; 24 hours) induces apoptosis in BaF3/WT and BaF3/T315I cells[1].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[3]. |
| Name | S116836 |
| CAS | 1257628-57-1 |
| Formula | C27H21F3N6O |
| Molar Mass | 502.49 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
S116836
CAS: 1257628-57-1 F: C27H21F3N6O W: 502.49
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116
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