An FLT3 inhibitor
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BPR1J-097

Item No. 29805

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-methyl-1-piperazinyl)-N-[5-[3-[(phenylsulfonyl)amino]phenyl]-1H-pyrazol-3-yl]-benzamide
CAS Number
1327167-19-0
Molecular Formula
C27H28N6O3S
Formula Weight
516.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:6): 0.14 mg/mlDMSO: 10 mg/ml
λmax
298 nm
SMILES
CN1CCN(C2=CC=C(C(NC3=NNC(C4=CC(NS(C5=CC=CC=C5)(=O)=O)=CC=C4)=C3)=O)C=C2)CC1
InChi Code
InChI=1S/C27H28N6O3S/c1-32-14-16-33(17-15-32)23-12-10-20(11-13-23)27(34)28-26-19-25(29-30-26)21-6-5-7-22(18-21)31-37(35,36)24-8-3-2-4-9-24/h2-13,18-19,31H,14-17H2,1H3,(H2,28,29,30,34)
InChi Key
RRKKHABFIOHAOI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $55

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    50 mg

    $242

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    100 mg

    $349

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    Product Description

    BPR1J-097 is an inhibitor of FMS-related tyrosine kinase 3 (FLT3; IC50 = 11 nM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lin, W.-H., Jiaang, W.-T., Chen, C.-W., et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br. J. Cancer 106(3), 475-481 (2012).