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

Tirbanibulin Mesylate (Synonyms: KX2-391 Mesylate; KX01 Mesylate)

Cat. No.: HY-10340B Purity: 99.88%
Handling Instructions

Tirbanibulin Mesylate (KX2-391 Mesylate) 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 Mesylate Chemical Structure

Tirbanibulin Mesylate Chemical Structure

CAS No. : 1080645-95-9

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10 mM * 1 mL in DMSO USD 93 In-stock
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10 mg USD 95 In-stock
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50 mg USD 350 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Tirbanibulin Mesylate:

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Description

Tirbanibulin Mesylate (KX2-391 Mesylate) 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, in HuH7 cells), 13 nM (Src, in PLC/PRF/5 cells), 26 nM (Src, in Hep3B cells), 60 nM (Src, in HepG2 cells)[1]

In Vitro

Tirbanibulin Mesylate (KX2-391 Mesylate) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (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 Mesylate (KX2-391 Mesylate) 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 Mesylate (KX2-391 Mesylate) 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].

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

In Vivo

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

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

Clinical Trial
Molecular Weight

527.63

Formula

C₂₇H₃₃N₃O₆S

CAS No.

1080645-95-9

SMILES

O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (189.53 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8953 mL 9.4763 mL 18.9527 mL
5 mM 0.3791 mL 1.8953 mL 3.7905 mL
10 mM 0.1895 mL 0.9476 mL 1.8953 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

TirbanibulinKX2-391KX01KX 01KX-01SrcMicrotubule/TubulinInhibitorinhibitorinhibit

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Product Name:
Tirbanibulin Mesylate
Cat. No.:
HY-10340B
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