[CAS NO. 1038395-65-1] Tirbanibulin dihydrochloride

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PRODUCTS SPECIFICATIONS [1038395-65-1]

Catalog

HY-10340A

Brand

MCE

CAS

1038395-65-1

DESCRIPTION [1038395-65-1]

Overview

MDL	MFCD20526429
Molecular Weight	504.45
Molecular Formula	C26H31Cl2N3O3
SMILES	O=C(CC1=NC=C(C2=CC=C(OCCN3CCOCC3)C=C2)C=C1)NCC4=CC=CC=C4.Cl.Cl

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

4 Publications Citing Use of MCE

Summary

Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) 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 HuH7), 13 nM (Src PLC/PRF/5), 26 nM (Src Hep3B), 60 nM (Src HepG2)

In Vitro

Tirbanibulin (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] . Tirbanibulin (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. Tirbanibulin (KX2-391) 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 (KX2-391) 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
NCT02838628	Almirall, S.A.\|Athenex, Inc.	Actinic Keratosis	April 11, 2016	Phase 2
NCT05231044	PharmaEssentia\|PharmaEssentia Japan K.K.	Actinic Keratosis	December 21, 2021	Phase 3
NCT02337205	Athenex, Inc.	Actinic Keratosis	December 2014	Phase 1
NCT05522816	PharmaEssentia\|Athenex, Inc.	Psoriasis	October 27, 2015	Phase 1
NCT05245578	PharmaEssentia\|PharmaEssentia Japan K.K.	Healthy Volunteer	November 16, 2021	Phase 1
NCT03285490	Almirall, S.A.\|Athenex, Inc.	Actinic Keratosis	September 15, 2017	Phase 3
NCT05279131	Almirall, S.A.	Keratosis, Actinic	June 28, 2022	Phase 3
NCT00646139	Roswell Park Cancer Institute	Lymphoma\|Lymphoproliferative Disorder\|Small Intestine Cancer\|Unspecified Adult Solid Tumor, Protocol Specific	October 2007	Phase 1
NCT05260073	Almirall, S.A.	Keratosis, Actinic	March 9, 2022
NCT01764087	Hanmi Pharmaceutical Company Limited	Unspecified Adult Solid Tumor, Protocol Specific\|Gastric Cancer\|Breast Cancer	December 2012	Phase 1\|Phase 2
NCT00658970	Athenex, Inc.	Solid Tumors\|Lymphoma	November 2007	Phase 1
NCT01074138	Kinex Pharmaceuticals Inc.\|Athenex, Inc.	Bone-Metastatic, Castration-Resistant Prostate Cancer	February 2010	Phase 2
NCT01397799	Kinex Pharmaceuticals Inc.\|Athenex, Inc.	Acute Myelogenous Leukemia	December 2013	Phase 1
NCT03285477	Almirall, S.A.\|Athenex, Inc.	Actinic Keratoses	September 18, 2017	Phase 3
NCT03575780	Athenex, Inc.\|TKL Research, Inc.	Actinic Keratoses	September 7, 2018	Phase 1
NCT05387525	Almirall, S.A.	Keratosis, Actinic	October 24, 2022	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

H ₂ O : 50 mg/mL ( 99.12 mM ; Need ultrasonic)

DMSO : 33.33 mg/mL ( 66.07 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9824 mL	9.9118 mL	19.8236 mL
5 mM	0.3965 mL	1.9824 mL	3.9647 mL
10 mM	0.1982 mL	0.9912 mL	1.9824 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 (4.96 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

* All of the co-solvents are available by MCE.