Art. -Nr.: HY-10340A

Tirbanibulin dihydrochloride

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

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

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.

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Reinheit: 98.02%
CAS. Nr.: 1038395-65-1
Formel: C₂₆H₃₁Cl₂N₃O₃
Molecular Weight:504.45

Speicherung:

4°C, stored under nitrogen

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

Tirbanibulin dihydrochloride Chemical Structure

CAS. Nr.: 1038395-65-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle Src Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 1038395-65-1
Appearance Solid
Molecular Weight 504.45
Formel C₂₆H₃₁Cl₂N₃O₃
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
Synonyms

KX2-391 dihydrochloride; KX-01 dihydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, stored under nitrogen

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

Publications (9)

All Cell Migration/Invasion AssayFlow CytometryCell Imaging/StainingWBCell Proliferation/Viability Assay

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Journal Impact Factor

Cancer Cell

PDGFRα+ITGA11+ fibroblasts foster early-stage cancer lymphovascular invasion and lymphatic metastasis via ITGA11-SELE interplay. [Abstract]

2024 Apr 8;42(4):682-700.e12. PMID: 38428409
Nat Commun

Defective N-glycosylation of IL6 induces metastasis and tyrosine kinase inhibitor resistance in lung cancer. [Abstract]

2024 Sep 9;15(1):7885. PMID: 39251588

Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 9;15(1):7885. [Abstract]

Effect of IL6 antibody (5 μg/mL), JAK-STAT3 inhibitors (S3I-201 = 10 μM, ruxolitinib = 2.5 μM), and SRC inhibitors (PP1 = 10 μM, PP2 = 10 μM, Tirbanibulin = 10 μM) on the migration of AS2-IL6-WT and AS2-IL6-N73Q cells through the space made by culture inserts. Images were obtained at 0 and 24 h.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Exp Clin Cancer Res

Genomic profiling of a collection of patient-derived xenografts and cell lines identified ixabepilone as an active drug against chemo-resistant osteosarcoma. [Abstract]

2025 Jul 8;44(1):195. PMID: 40624718
Microbiol Spectr

Repurposing flufenamic acid as a putative PmrB-directed adjuvant to restore colistin activity in Klebsiella pneumoniae. [Abstract]

2026 Mar 17:e0362025. PMID: 41842337
J Biol Chem

Reversible binding of the anticancer drug KXO1 (tirbanibulin) to the colchicine-binding site of β-tubulin explains KXO1's low clinical toxicity. [Abstract]

2019 Nov 29;294(48):18099-18108. PMID: 31628188

Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 0, 12.5, 25, 50, 100 nM; 16 h) induced cell cycle arrest at G2/M phase in HeLa, HepG2, and H460 cells.

Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

HeLa cells were treated with 100 nM paclitaxel (PTX), 100 nM vinblastine (Vin), 100 nM colchicine (Col), or 30 or 100 nM Tirbanibulin(KXO1) for 16 h, and microtubule morphology was monitored by immunofluorescence.

Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 1 5 25 nM; 16 h) was incubated for 2 h before being treated with 100 μM EBI for another 2 h. Tirbanibulin inhibited the formation of the EBI-tubulin complex, but vinblastine did not, thus confirming KXO1 binding to the colchicine site on tubulin.

Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 0-10000 nM; 5 days) reduced cell viability at 100000 nM in HeLa cells.

Tirbanibulin dihydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Nov 29;294(48):18099-18108. [Abstract]

Tirbanibulin (KXO1; 0-10000 nM; 10 h) was a totally reversible tubulin inhibitor.
Brain Res

Donepezil promotes neurogenesis via Src signaling pathway in a rat model of chronic cerebral hypoperfusion. [Abstract]

2020 Jun 1:1736:146782. PMID: 32184165
University of Colorado Denver

2024.
bioRxiv

2023 Dec 14.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 100 mg/mL (198.24 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9824 mL

9.9118 mL

19.8236 mL

5 mM

0.3965 mL

1.9824 mL

3.9647 mL

10 mM

0.1982 mL

0.9912 mL

1.9824 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Protokoll

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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474. [Content Brief]

[2]. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
H₂O	100 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.4956 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.

Keywords

Tirbanibulin dihydrochloride

9 Cited Publications

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Tirbanibulin dihydrochloride

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Publications Citing Use of MedChemExpress (MCE) Tirbanibulin dihydrochloride

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tirbanibulin dihydrochloride Related Classifications

HY-10340A Related Classifications