1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

Motixafortide (Synonyms: BKT140 (4-fluorobenzoyl); BL-8040; TF14016)

Cat. No.: HY-P0171 Purity: 99.19%
Handling Instructions

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.

For research use only. We do not sell to patients.

Motixafortide Chemical Structure

Motixafortide Chemical Structure

CAS No. : 664334-36-5

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1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
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Description

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.

IC50 & Target[1]

CXCR4

∼1 nM (IC50)

In Vitro

Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide (BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140) specifically triggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulates apoptotic cell death in leukemia and MM cells[2].

In Vivo

Subcutaneous injections of Motixafortide (BKT140) significantly reduces, in a dose-dependent manner, the growth of human acute myeloid leukemia and multiple myeloma xenografts. Tumors from animals treated with Motixafortide (BKT140) are smaller in size and weights, had larger necrotic areas and high apoptotic scores[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 36 mg/mL (16.67 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.4631 mL 2.3153 mL 4.6307 mL
5 mM 0.0926 mL 0.4631 mL 0.9261 mL
10 mM 0.0463 mL 0.2315 mL 0.4631 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) or AMD3100 for 24 hours. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of 2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH. Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37°C for 1 hour, and inactivated by heat treatment (65°C for 30 minutes). After incubation, cells are stained with propidium iodide and the percent of viable PI-negative cells in culture is determined[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Severe combined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study. NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 mL per mouse containing 5×106 cells). Tumor growth is monitored daily, and mice are randomized to drug-treated or control PBS-treated groups (10 mice per group) when the tumor size (width×length) reaches 0.04 cm2. BKT140 is administered subcutaneously at a dose of 200 mg per mouse each day for 5 days[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

2159.52

Formula

C₉₇H₁₄₄FN₃₃O₁₉S₂

CAS No.

664334-36-5

Sequence

4F-Benzoyl-Arg-Arg-{2-Naph-Ala}-Cys-Tyr-{Cit}-Lys-Lys-Pro-Tyr-Arg-{Cit}-Cys-Arg-NH2 (Disulfide bridge: Cys4-Cys13)

Sequence Shortening

4F-Benzoyl-RR-{2-Naph-Ala}-CY-{Cit}-KKPYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13)

SMILES

[4F-Benzoyl-RR-{2-Naph-Ala}-CY-{Cit}-KKPYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13)]

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Motixafortide
Cat. No.:
HY-P0171
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Motixafortide

Cat. No.: HY-P0171