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

BPR1J-097 – 10 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.  

 

Available on backorder

Add to quotes
SKU: 29805 - 10 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

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 100 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 25 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 100 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 100 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page