Motixafortide TFA(664334-36-5,Free) 是 CXCR4 的拮抗剂，IC50 为 ～1 nM。它通过改变 miR-15a/16-1 表达下调 ERK、BCL-2、MCL-1 和 cyclin-D1 来诱导 AML 原始细胞凋亡。

Motixafortide is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Treatment with BL-8040 induces the robust mobilization of AML blasts from the BM. In addition, AML cells exposed to BL-8040 undergoes differentiation. BL-8040 induces the apoptosis of AML cells in vitro, which is mediated by the up-regulation of miR-15a/miR-16-1, resulting in down-regulation of the target genes BCL-2, MCL-1 and cyclin-D1. Overexpression of miR-15a/miR-16-1 directly induces leukemic cell death. BL-8040-induced apoptosis is also mediated by the inhibition of survival signals via the AKT/ERK pathways.

BL-8040 also synergizes with FLT3 inhibitors to induce AML cell death. Importantly, this combined treatment prolongs the survival of tumor-bearing mice and reduces minimal residual disease in vivo.

T14665L

C99H145F4N33O21S2

2273.54

BKT140 TFA;TF 14016 TFA;T140 TFA;BL-8040 TFA

H2O:100 mg/mL (46.31 mM),need ultrasonic
DMSO:100 mg/mL (46.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years