protac flt3 degrader 1

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.

PROTACFLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader targeting FLT3, JAK2, and BRD4, with DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It exhibits potent antiproliferative activity against MV4;11 cells (IC50= 0.79 nM) and FLT3-mutated Ba/F3 cells. Additionally, PROTACFLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells and demonstrates significant antitumor efficacy in an MV4;11 xenograft model established in NOD SCID mice. This compound is applicable for research in acute myeloid leukemia (AML).

PROTACFLT3/CHK1 Degrader-1 is a PROTAC agent targeting FLT3 and CHK1, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1). It inhibits the phosphorylation of downstream signaling effectors STAT5(Tyr694), AKT(Ser473), and ERK(Tyr204) of FLT3, reduces c-Myc protein levels, and maintains p53 protein expression. Additionally, PROTACFLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells and demonstrates significant antitumor activity in mice with MV-4-11 xenografts. This compound is applicable in acute myeloid leukemia (AML) research.

PROTAC FLT3/CDK9 degrader-1, a potent dual degrader of FLT3 and CDK9, effectively induces apoptosis and targets protein degradation of FLT3 and CDK9. This compound holds research potential for FLT3-ITD mutated AML [1].

PROTACFLT3/CDKs degrader-1 (Compound C3) is an agent that degrades cyclin-dependent kinase (CDK2 with a DC50 of 18.73 nM) and FMS-like tyrosine kinase 3 (FLT3). It induces differentiation in HL-60 cells, achieving a 72.77% differentiation rate at 6.25 nM, and inhibits proliferation of acute myeloid leukemia (AML) cells, with an IC50 ranging from 2.9 to 37 nM. PROTACFLT3/CDKs degrader-1 demonstrates potential for improving the treatment of AML.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.

FLT3 ligand-2 serves as a ligand for the target protein in PROTAC. It is utilized for synthesizing PROTAC FLT-3 degrader 1.

FLT3/JAK2/BRD4 ligand-1 is a ligand for FLT3, JAK2, and BRD4. It serves as a component for synthesizing PROTAC [FLT3/JAK2/BRD4 Degrader-1].

FLT3/CHK1 ligand-1 is a PROTAC target protein ligand used in the synthesis of PROTACs, such as [PROTAC FLT3/CHK1 Degrader-1]. [PROTAC FLT3/CHK1 Degrader-1] functions as a potent FLT3/CHK1 PROTAC degrader with antitumor activity.

PF15, a selective FLT3-ITD degrader, serves as a PROTAC (proteolysis targeting chimera) tethering ligands for FLT3 kinase and CRBN. It exhibits a degradation concentration 50 (DC50) of 76.7 nM and notably impedes the proliferation of FLT3-ITD-positive cells. PF15 also reduces phosphorylation levels of FLT3 and STAT5 and demonstrates efficacy in inhibiting tumor growth in mouse models, suggesting potential applications in leukemia research [1].

FLT3/CDKs ligand-1 (Compound 14) functions as a ligand for target proteins, promoting the degradation of Cyclin-Dependent Kinases (CDK) and FMS-like tyrosine kinase 3 (FLT3), thereby inhibiting the proliferation and survival of leukemia cells associated with FLT3/CDK. This compound is also used in the synthesis of PROTAC FLT3/CDKs Degrader-1.