SEL24-B489 是有效的、I 型的、口服有效的、PIM 和 FLT3-ITD 的双抑制剂，其对PIM1、PIM2 和 PIM3 的 K_d 值分别为 2 nM、2 nM、和 3 nM。

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

Solid

PIM1 2 nM (Kd) PIM2 2 nM (Kd)

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.
SEL24-B489 causes a profound inhibition of S6 (S), but has little effect on PI3K/mTOR signaling.
SEL24-B489 inhibits STAT5 (Ser) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage.
has not independently confirmed the accuracy of these methods. They are for reference only.

SEL24-B489 (25-100 mg/kg, orally) exhibited activity in AML in vivo models.
SEL24-B489 induces apoptosis of DLBCL cell lines in low/sub-micromolar concentrations and exhibits activity in a xenograft model.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Wojciech Czardybon, A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia. Oncotarget. 2018 Mar 30;9(24):16917-16931.
[2]. Ewa Jablonska, et al. A Novel Pan-PIM Kinase Inhibitor, SEL24-B489, Induces Apoptosis and Inhibits Proliferation of Diffuse Large B-Cell Lymphoma Cells through Inhibition of Protein Translation and Attenuation of Myc and NFkB Activity. Blood (2015) 126 (2

In Vitro: DMSO : 25 mg/mL (56.04 mM; ultrasonic and adjust pH to 2 with HCl)配制储备液