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Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) 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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $297 | In Stock | |
25 mg | $475 | In Stock | |
50 mg | $672 | In Stock | |
100 mg | $893 | In Stock | |
200 mg | $1,180 | In Stock |
Description | Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) 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. |
Targets&IC50 | CXCR4:~1 nM |
In vitro | Treatment with Motixafortide induces the robust mobilization of AML blasts from the BM. In addition, AML cells exposed to Motixafortide undergoes differentiation. Motixafortide 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. Motixafortide-induced apoptosis is also mediated by the inhibition of survival signals via the AKT/ERK pathways. |
In vivo | Motixafortide 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. |
Alias | TF 14016 TFA, T140 TFA, BL-8040 TFA, BKT140 TFA |
Molecular Weight | 2273.54 |
Formula | C99H145F4N33O21S2 |
Smiles | FC(F)(F)C(O)=O.C1C[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2C1)CCCCN)CCCCN)CCCNC(=O)N)CC3=CC=C(C=C3)O)NC(=O)[C@H](CC4=CC5=CC=CC=C5C=C4)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C6=CC=C(C=C6)F)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N)CCCNC(=O)N)CCCNC(=N)N)CC7=CC=C(C=C7)O |
Relative Density. | no data available |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | H2O: 100 mg/mL (46.31 mM), Sonication is recommended. DMSO: 100 mg/mL (46.31 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
H2O/DMSO
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