[CAS NO. 1080645-95-9] Tirbanibulin Mesylate

Name: Tirbanibulin Mesylate
Brand: Arctom Scientific
SKU: AS941519

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PRODUCTS SPECIFICATIONS [1080645-95-9]

Distributor

Catalog

AS941519

Brand

Arctom Scientific

CAS

1080645-95-9

DESCRIPTION [1080645-95-9]

Overview

MDL	MFCD30496706
Molecular Weight	527.63
Molecular Formula	C27H33N3O6S
SMILES	O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2.CS(=O)(O)=O

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

Tirbanibulin Mesylate (KX2-391 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src , with GI ₅₀ 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 (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] . 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 GI ₅₀ 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05522816	PharmaEssentia\|Athenex, Inc.	Psoriasis	October 27, 2015	Phase 1
NCT05231044	PharmaEssentia\|PharmaEssentia Japan K.K.	Actinic Keratosis	December 21, 2021	Phase 3
NCT05279131	Almirall, S.A.	Keratosis, Actinic	June 28, 2022	Phase 3
NCT03285477	Almirall, S.A.\|Athenex, Inc.	Actinic Keratoses	September 18, 2017	Phase 3
NCT05245578	PharmaEssentia\|PharmaEssentia Japan K.K.	Healthy Volunteer	November 16, 2021	Phase 1
NCT00658970	Athenex, Inc.	Solid Tumors\|Lymphoma	November 2007	Phase 1
NCT05260073	Almirall, S.A.	Keratosis, Actinic	March 9, 2022
NCT03575780	Athenex, Inc.\|TKL Research, Inc.	Actinic Keratoses	September 7, 2018	Phase 1
NCT00646139	Roswell Park Cancer Institute	Lymphoma\|Lymphoproliferative Disorder\|Small Intestine Cancer\|Unspecified Adult Solid Tumor, Protocol Specific	October 2007	Phase 1
NCT01074138	Kinex Pharmaceuticals Inc.\|Athenex, Inc.	Bone-Metastatic, Castration-Resistant Prostate Cancer	February 2010	Phase 2
NCT03285490	Almirall, S.A.\|Athenex, Inc.	Actinic Keratosis	September 15, 2017	Phase 3
NCT02337205	Athenex, Inc.	Actinic Keratosis	December 2014	Phase 1
NCT05387525	Almirall, S.A.	Keratosis, Actinic	October 24, 2022	Phase 4
NCT01764087	Hanmi Pharmaceutical Company Limited	Unspecified Adult Solid Tumor, Protocol Specific\|Gastric Cancer\|Breast Cancer	December 2012	Phase 1\|Phase 2
NCT01397799	Kinex Pharmaceuticals Inc.\|Athenex, Inc.	Acute Myelogenous Leukemia	December 2013	Phase 1
NCT02838628	Almirall, S.A.\|Athenex, Inc.	Actinic Keratosis	April 11, 2016	Phase 2

Appearance

Solid

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 available by MCE.