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

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

Cat. No.: HY-P0171 Purity: 99.88%
SDS COA 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.

Custom Peptide Synthesis

Motixafortide Chemical Structure

Motixafortide Chemical Structure

CAS No. : 664334-36-5

Size Price Stock Quantity
5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 900 In-stock
50 mg USD 1450 In-stock
100 mg USD 2300 In-stock
200 mg   Get quote  
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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].

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

Clinical Trial
Molecular Weight

2159.52

Formula

C97H144FN33O19S2

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

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

Sequence Shortening

{4-Fluorobenzoyl}-RR-{2-Naph-Ala}-CY-{Cit}-K-{d-Lys}-PYR-{Cit}-CR-NH2 (Disulfide bridge: Cys4-Cys13)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (46.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 50 mg/mL (23.15 mM; Need ultrasonic)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 110 mg/mL (50.94 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.88%

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 μL 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 μg per mouse each day for 5 days[2].

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

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 0.4631 mL 2.3153 mL 4.6307 mL 11.5766 mL
5 mM 0.0926 mL 0.4631 mL 0.9261 mL 2.3153 mL
10 mM 0.0463 mL 0.2315 mL 0.4631 mL 1.1577 mL
15 mM 0.0309 mL 0.1544 mL 0.3087 mL 0.7718 mL
20 mM 0.0232 mL 0.1158 mL 0.2315 mL 0.5788 mL
DMSO 25 mM 0.0185 mL 0.0926 mL 0.1852 mL 0.4631 mL
30 mM 0.0154 mL 0.0772 mL 0.1544 mL 0.3859 mL
40 mM 0.0116 mL 0.0579 mL 0.1158 mL 0.2894 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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