Home Angiogenesis Src inhibitor Tirbanibulin

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Tirbanibulin Src inhibitor

Cat.No.S2700

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 Src inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 431.53

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 431.53 Formula

C26H29N3O3

 Storage (From the date of receipt)
CAS No. 897016-82-9 Download SDF Storage of Stock Solutions

Synonyms KX2-391,KX 01 Smiles C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (199.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Src (HuH7) [1]
(Cell-free assay)
9 nM(GI50)
Src (PLC/PRF/5) [1]
(Cell-free assay)
13 nM(GI50)
Src (Hep 3B) [1]
(Cell-free assay)
26 nM(GI50)
Src (Hep G2) [1]
(Cell-free assay)
60 nM(GI50)
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]
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]
References

Applications

Methods Biomarkers Images PMID
Western blot α-SMA / Collagen 1 / Fibronectin / p-Src / Src S2700-WB1 29137389

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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

Tech Support

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Frequently Asked Questions

Question 1:
How to formulate it for animal trials?

Answer:
It 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.

Signaling Pathway Map