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PROTACFLT3/GSPT1/IKZF1/3 degrader-1 is an FLT3 PROTAC degrader with DC50 = 1.2 nM. It functions as a molecular glue to degrade its brain substrates and exhibits antiproliferative activity against resistant acute myeloid leukemia (AML) cells, showing potential applications in AML research.
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| Description | PROTACFLT3/GSPT1/IKZF1/3 degrader-1 is an FLT3 PROTAC degrader with DC50 = 1.2 nM. It functions as a molecular glue to degrade its brain substrates and exhibits antiproliferative activity against resistant acute myeloid leukemia (AML) cells, showing potential applications in AML research. |
| In vitro | PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 (Compound A2) exhibits antiproliferative activity against MV-4-11 FLT3-ITD, MV-4-11 FLT3-ITD-F691L, MV-4-11 FLT3-ITD-D835Y, MOLM-13 FLT3-ITD, MOLM-13 FLT3-ITD-F691L, and MOLM-13-D835Y, with IC50 values of 1.67, 4.74, 3.70, 3.16, 5.61, and 7.55 nM, respectively, while showing no effect on the proliferation of FLT3 wild-type cells (IC50 > 1000). At concentrations of 0-100 nM over 24 hours, PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 reduces the expression of FLT3, GSPT1, IKZF1, and IKZF3 proteins in MV-4-11 and MOLM-13 cells. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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