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

BKT140 ​(4-​fluorobenzoyl) (Synonyms: BL-8040; TF14016; 4F-Benzoyl-TN14003)

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

BKT140 is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.

For research use only. We do not sell to patients.
BKT140 ​(4-​fluorobenzoyl) Chemical Structure

BKT140 ​(4-​fluorobenzoyl) Chemical Structure

CAS No. : 664334-36-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1140 In-stock
1 mg USD 132 In-stock
5 mg USD 396 In-stock
10 mg USD 600 In-stock
25 mg USD 1200 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BKT140 is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.

IC50 & Target

IC50: ~1 nM (CXCR4)[1].

In Vitro

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

In Vivo

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

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[2]

Hematopoietic cancer cells are incubated with different concentrations of BKT140 or AMD3100 for 24 hours. 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 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]

BKT140 is prepared in PBS.

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

SMILES

[4F-Benzoyl-RRACYXKKPYRXCR]

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 36 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BKT140 ​(4-​fluorobenzoyl)
Cat. No.:
HY-P0171
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