[CAS NO. 948557-43-5] Tie2 kinase inhibitor 1

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PRODUCTS SPECIFICATIONS [948557-43-5]

Catalog

HY-100556

Brand

MCE

CAS

948557-43-5

DESCRIPTION [948557-43-5]

Overview

MDL	MFCD18384977
Molecular Weight	439.53
Molecular Formula	C26H21N3O2S
SMILES	O=S(C1=CC=C(C2=NC(C3=CC=NC=C3)=C(C4=CC=C5C=C(OC)C=CC5=C4)N2)C=C1)C

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

1 Publications Citing Use of MCE

[1]Patent. US20170349880A1.

Summary

Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC ₅₀ of 250 nM ^[1] . Tie2 kinase inhibitor 1 has anti-cancer activity ^[2] .

IC50 & Target

IC50: 250 nM (Tie2) ^[1]

In Vitro

Tie2 kinase inhibitor 1 (compound 5) has an IC ₅₀ of 50 μM for p38 and has moderate to excellent cellular activities (cell IC ₅₀ =232 nM) ^[1] .
Tie2 kinase inhibitor 1 inhibits tunica internal endothelial cell kinase 2 (Tie2) ^[2] .

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

In Vivo

Tie2 kinase inhibitor 1 (intraperitoneally; 50 mg/kg; twice a week for 6 weeks) results in statistically significant reductions in tumor volume by day 15. Tie2 kinase inhibitor 1 results in a 61% reduction in tumor volume by day 20, and reduces tumor volume by 45% by 6 weeks ^[1] .

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

Animal Model:	Athymic nude mice (6- to 8-week-old females) ^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneally; twice a week for 6 weeks
Result:	Resulted in statistically significant reductions in tumor volume.

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 : 17.86 mg/mL ( 40.63 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2752 mL	11.3758 mL	22.7516 mL
5 mM	0.4550 mL	2.2752 mL	4.5503 mL
10 mM	0.2275 mL	1.1376 mL	2.2752 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: ≥ 1.79 mg/mL (4.07 mM); Clear solution
2.

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

Solubility: ≥ 1.79 mg/mL (4.07 mM); Clear solution

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