2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage
  3. Src Microtubule/Tubulin
  4. Tirbanibulin dihydrochloride

Tirbanibulin dihydrochloride  (Synonyms: KX2-391 dihydrochloride; KX-01 dihydrochloride)

Cat. No.: HY-10340A Purity: 99.59%
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Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

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

Tirbanibulin dihydrochloride Chemical Structure

Tirbanibulin dihydrochloride Chemical Structure

CAS No. : 1038395-65-1

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Based on 7 publication(s) in Google Scholar

Other Forms of Tirbanibulin dihydrochloride:

Tirbanibulin dihydrochloride Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

IC50 & Target

GI50: 9 nM (Src HuH7), 13 nM (Src PLC/PRF/5), 26 nM (Src Hep3B), 60 nM (Src HepG2)
In Vitro

Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines[1]. Tirbanibulin (KX2-391) is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. Tirbanibulin (KX2-391) is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively[2].

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

Tirbanibulin dihydrochloride Related Antibodies
In Vivo

Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer[2].

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

504.45

Formula

C26H31Cl2N3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (99.12 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (66.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9824 mL 9.9118 mL 19.8236 mL
5 mM 0.3965 mL 1.9824 mL 3.9647 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 (stored under nitrogen). 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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
References
Cell Assay
[1]

Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37°C and 5% CO2. Cells are seeded at 4.0×103/190 μL and 8.0×103/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37°C and 5% CO2 prior to the addition of Tirbanibulin (KX2-391), at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten μLs of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured. For comparison of activity and potency, parallel experiments are performed using Tirbanibulin (KX2-391). Growth inhibition curves, 50% inhibition concentration (GI50), and 80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format.

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 (stored under nitrogen). 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
DMSO / H2O 1 mM 1.9824 mL 9.9118 mL 19.8236 mL 49.5589 mL
5 mM 0.3965 mL 1.9824 mL 3.9647 mL 9.9118 mL
10 mM 0.1982 mL 0.9912 mL 1.9824 mL 4.9559 mL
15 mM 0.1322 mL 0.6608 mL 1.3216 mL 3.3039 mL
20 mM 0.0991 mL 0.4956 mL 0.9912 mL 2.4779 mL
25 mM 0.0793 mL 0.3965 mL 0.7929 mL 1.9824 mL
30 mM 0.0661 mL 0.3304 mL 0.6608 mL 1.6520 mL
40 mM 0.0496 mL 0.2478 mL 0.4956 mL 1.2390 mL
50 mM 0.0396 mL 0.1982 mL 0.3965 mL 0.9912 mL
60 mM 0.0330 mL 0.1652 mL 0.3304 mL 0.8260 mL
H2O 80 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6195 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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Tirbanibulin dihydrochloride Related Classifications

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.

Keywords:

Tirbanibulin1038395-65-1KX2-391KX-01KX01KX 01SrcMicrotubule/TubulinInhibitorinhibitorinhibit

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