For research use only.
Catalog No.S9665 Synonyms: BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140
CAS No. 664334-36-5
Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
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|Description||Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 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. 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.
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.
|In vitro||Water||100 mg/mL (46.3 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02763384||Recruiting||Drug: BL-8040|Drug: Nelarabine||T-Acute Lymphoblastic Leukemia|Adult T Lymphoblastic Lymphoma||Washington University School of Medicine|The Leukemia and Lymphoma Society|National Institutes of Health (NIH)|National Cancer Institute (NCI)||December 2 2016||Phase 2|
|NCT02115672||Withdrawn||Drug: BL-8040||Chronic Myeloid Leukemia||Sheba Medical Center||November 2014||Phase 1|Phase 2|
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