1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Pim
    FLT3
    Apoptosis
  3. SEL24-B489

SEL24-B489 

Cat. No.: HY-120758
Handling Instructions

SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.

For research use only. We do not sell to patients.

SEL24-B489 Chemical Structure

SEL24-B489 Chemical Structure

CAS No. : 1616359-00-2

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Description

SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively[1].

IC50 & Target[1]

PIM1

2 nM (Kd)

PIM2

2 nM (Kd)

PIM3

3 nM (Kd)

FLT3-ITD

 

In Vitro

In MOLM-13 and to a lesser extent in MV4-11 cells, a dose-dependent disruption of cell cycle with especially pronounced depletion of the S phase after treatment with SEL24-B489, accompanied by PARP cleavage and apoptosis was observed[1].
SEL24-B489 causes a profound inhibition of S6 (S235/236), but has little effect on PI3K/mTOR signaling[1].
SEL24-B489 inhibits STAT5 (Ser726) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: AZD1208, AC220 and AraC in AML cell lines.
Concentration: 0-10 μM.
Incubation Time: 72 h.
Result: Decreased viability.
In Vivo

SEL24-B489 (25-100 mg/kg, orally) exhibited activity in AML in vivo models[1].
SEL24-B489 induces apoptosis of DLBCL cell lines in low/sub-micromolar concentrations and exhibits activity in a xenograft model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID/beige mice bearing MV-4-11 tumors (FLT3-ITD+)[1].
Dosage: 50, 75 and 100 mg/kg.
Administration: Orally, twice daily.
Result: Marked dose – dependent tumor reduction (67%, 74% and 82% tumor growth inhibition (TGI) for 50, 75 and 100 mg/kg daily doses, respectively).
Molecular Weight

446.14

Formula

C₁₅H₁₈Br₂N₄O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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SEL24-B489
Cat. No.:
HY-120758
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