[CAS NO. 910634-41-2] Litronesib

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PRODUCTS SPECIFICATIONS [910634-41-2]

Catalog

HY-14846

Brand

MCE

CAS

910634-41-2

DESCRIPTION [910634-41-2]

Overview

MDL	MFCD19442197
Molecular Weight	511.70
Molecular Formula	C23H37N5O4S2
SMILES	CC(C)(C)C(N1[C@@](C2=CC=CC=C2)(CNS(CCNCC)(=O)=O)SC(NC(C(C)(C)C)=O)=N1)=O

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

Summary

Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity ^[1] .

IC50 & Target

Eg5

In Vitro

Litronesib (LY2523355) is a selective Eg5 inhibitor. Litronesib (25 nM) induces cancer cells to death during mitotic arrest, and this needs sustained activation of spindle-assembly checkpoint (SAC) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Litronesib (LY2523355; 1.1, 3.3, 10, and 30 mg/kg, i.v.) shows antitumor activity in a dose-dependently, and causes a dramatic increase in cancer cells immuno-positive for histone H3 phosphorylation in Colo205 xenograft tumors ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01059643	Eli Lilly and Company	Ovarian Cancer\|Non Small Cell Lung Cancer\|Prostate Cancer\|Colorectal Cancer\|Gastric Cancer\|Esophageal Cancer\|Cancer of Head and Neck	April 2011	Phase 2
NCT01214642	Eli Lilly and Company	Advanced Cancer	May 2008	Phase 1
NCT01358019	Kyowa Kirin Co., Ltd.	Solid Tumors	May 2011	Phase 1
NCT01214629	Eli Lilly and Company	Advanced Cancer\|Metastatic Cancer	July 2007	Phase 1
NCT01025284	Eli Lilly and Company	Small Cell Lung Cancer	December 2009	Phase 2
NCT01214655	Eli Lilly and Company	Acute Leukemia	June 2008	Phase 1
NCT01416389	Eli Lilly and Company	Metastatic Breast Cancer	August 2011	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL ( 97.71 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9543 mL	9.7713 mL	19.5427 mL
5 mM	0.3909 mL	1.9543 mL	3.9085 mL
10 mM	0.1954 mL	0.9771 mL	1.9543 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 (4.89 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (4.89 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (4.89 mM); Clear solution

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

References

[1] Ye XS, et al. A Novel Eg5 Inhibitor (LY2523355) Causes Mitotic Arrest and Apoptosis in Cancer Cells and Shows Potent Antitumor Activity in Xenograft Tumor Models. Mol Cancer Ther. 2015 Nov;14(11):2463-72.