An FLT3 inhibitor (IC50 = 11 nM); selective for FLT3 over FLT1

BPR1J-097 – 50 mg

Brand:
Cayman
CAS:
1327167-19-0
Storage:
-20
UN-No:
Non-Hazardous - /

BPR1J-097 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50 = 11 nM).{46746} It is selective for FLT3 over FLT1, KDR, Aurora A, and Aurora B kinases (IC50s = 211, 129, 340, and 876 nM, respectively). BPR1J-097 inhibits FLT3 activity and phosphorylation of STAT5 in MV4-11 acute myeloid leukemia (AML) cells containing the FLT3 activating mutant FLT3-ITD (IC50s = 10 and 1 nM, respectively). It inhibits the growth of FLT3-dependent MOLM-13 and MV4-11 AML cells (GI50s = 21 and 46 nM, respectively) but not FLT3-/- U937 and K562 cells (GI50s = >20,000 nM for both). BPR1J-097 (25 mg/kg) inhibits tumor growth in a MOLM-13 mouse xenograft model.  

 

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SKU: 29805 - 50 mg Category:

Description

An FLT3 inhibitor (IC50 = 11 nM); selective for FLT3 over FLT1, KDR, Aurora A, and Aurora B kinases (IC50s = 211, 129, 340, and 876 nM, respectively); inhibits FLT3 activity and phosphorylation of STAT5 in MV4-11 AML cells containing the FLT3 activating mutant FLT3-ITD (IC50s = 10 and 1 nM, respectively); inhibits the growth of FLT3-dependent MOLM-13 and MV4-11 AML cells (GI50s = 21 and 46 nM, respectively); inhibits tumor growth in a MOLM-13 mouse xenograft model at 25 mg/kg

Formal name: 4-(4-methyl-1-piperazinyl)-N-[5-[3-[(phenylsulfonyl)amino]phenyl]-1H-pyrazol-3-yl]-benzamide

Synonyms: 

Molecular weight: 516.6

CAS: 1327167-19-0

Purity: ≥95%

Formulation: A crystalline solid

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