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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.
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Quality Control

Batch: Purity: 99.95%
99.95

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

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
Dilution Calculator Molecular Weight Calculator

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
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%

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.

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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

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

In vivo

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

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 2025-09-17)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07010692 RECRUITING
Keratinocyte Carcinoma; Basal Cell Carcinomas; Squamous Cell Carcinoma; Skin Cancer
Bruce Robinson, MD
2025-05-16 PHASE1; PHASE2
NCT07273656 NOT_YET_RECRUITING
Keratosis; Actinic Keratoses
University Hospital, Lille
2026-11-30 PHASE3
NCT06112522 RECRUITING
Cell Carcinoma
Centre Hospitalier Universitaire de Nice
2024-02-16 PHASE2
NCT05387525 ACTIVE_NOT_RECRUITING
Keratosis, Actinic
Almirall, S.A.
2022-10-24 PHASE4
NCT06791525 RECRUITING
Warts Hand
The Skin Center Dermatology Group
2025-05-01 PHASE4
NCT06135415 COMPLETED
Keratosis, Actinic
Almirall, S.A.
2023-12-21 PHASE3

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Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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.

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