Information Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist ofCXCR4with IC50 of ～1 nM. BL-8040 induces theapoptosisof AML blasts by down-regulatingERK,BCL-2,MCL-1andcyclin-D1via altered miR-15a/16-1 expression. Targets ERK ; Bcl-2 ; MCL-1 ; cyclin-D1 ; CXCR4 (Cell-free assay) ; 1 nM In vitro 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. This apoptosis 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. In vivo BL-8040 induces the apoptosis of AML cells in vivo. Treatment with a BCL-2 inhibitor induces apoptosis and acts together with BL-8040 to enhance cell death. 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. Cell Research(from reference) Cell lines：The leukemic cell lines (MV4-11, THP-1, U937, HL-60) Concentrations：0.1 μM, 1 μM, 10 μM, 20 μM Incubation Time：24 h, 48 h
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Motixafortide (BL-8040)
CAS number：664334-36-5 molecular formula：C97H144FN33O19S2
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| Chinese alias | - | ||
| English alias | CHEBI:145536 | L-ARGININAMIDE, N2-(4-FLUOROBENZOYL)-L-ARGINYL-L-ARGINYL-3-(2-NAPHTHALENYL)-L-ALANYL-L-CYSTEINYL-L-TYROSYL-N5-(AMINOCARBONYL)-L-ORNITHYL-L-LYSYL-D-LYSYL-L-PROLYL-L-TYROSYL-L-ARGINYL-N5-(AMINOCARBONYL)-L-ORNITHYL-L-CYSTEINYL-, CYCLIC (4->13) | ||
| CAS number | 664334-36-5 | molecular formula | C97H144FN33O19S2 |
| molecular weight | 2159.52 g/mol | Exact mass | - |
| PSA | - | logp | -3.895 |
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