Tirbanibulin

Synonyms: KX 01

Tirbanibulin, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.

Tirbanibulin Chemical Structure

Tirbanibulin Chemical Structure

CAS: 897016-82-9

Selleck's Tirbanibulin has been cited by 36 publications

Purity & Quality Control

Batch: Purity: 99.95%
99.95

Tirbanibulin Related Products

Signaling Pathway

Choose Selective Src Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse NIH3T3 cells Function assay 3 days Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay 21852023
Click to View More Cell Line Experimental Data

Biological Activity

Description Tirbanibulin, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
Targets
Src (HuH7) [1]
(Cell-free assay)
Src (PLC/PRF/5) [1]
(Cell-free assay)
Src (Hep 3B) [1]
(Cell-free assay)
Src (Hep G2) [1]
(Cell-free assay)
9 nM(GI50) 13 nM(GI50) 26 nM(GI50) 60 nM(GI50)
In vitro
In vitro

KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. [1] 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. 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]

Cell Research Cell lines Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines
Concentrations 6,564 to 0.012 nM
Incubation Time 3 days
Method

Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 (NutriCyte, Buffalo, NY) 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 KX2-391, at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten microliters 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 by using BioTek Synergy HT multiplatform microplate reader. For comparison of activity and potency, parallel experiments are performed using 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.

Experimental Result Images Methods Biomarkers Images PMID
Western blot α-SMA / Collagen 1 / Fibronectin / p-Src / Src 29137389
In Vivo
In vivo

In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. [2]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06112522 Not yet recruiting
Cell Carcinoma
Centre Hospitalier Universitaire de Nice
December 1 2023 Phase 2
NCT05900258 Completed
Actinic Keratosis
Medical University of Graz
May 11 2023 Phase 4
NCT05741294 Completed
Actinic Keratosis
Almirall S.A.
January 17 2023 Phase 4
NCT03575780 Completed
Actinic Keratoses
Athenex Inc.|TKL Research Inc.
September 7 2018 Phase 1
NCT02838628 Completed
Actinic Keratosis
Almirall S.A.|Athenex Inc.
April 11 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 431.53 Formula

C26H29N3O3

CAS No. 897016-82-9 SDF Download Tirbanibulin SDF
Smiles C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (199.29 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
How to formulate KX2-391 for animal trials?

Answer:
KX2-391 can be dissolved in 4% DMSO/corn oil at 5 mg/ml as a homogeneous suspension for oral administration and dissolved in 4% DMSO/30% PEG 300/ddH2O at 5 mg/ml as a clear solution.

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