[CAS NO. 227963-15-7] MK-0429

Name: MK-0429
Brand: Arctom Scientific
SKU: AS093572

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PRODUCTS SPECIFICATIONS [227963-15-7]

Distributor

Catalog

AS093572

Brand

Arctom Scientific

CAS

227963-15-7

DESCRIPTION [227963-15-7]

Overview

MDL	MFCD27665469
Molecular Weight	439.51
Molecular Formula	C23H29N5O4
SMILES	O=C1N([C@H](C2=CC=C(OC)N=C2)CC(O)=O)CCN1CCCC3=NC4=C(C=C3)CCCN4

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

2 Publications Citing Use of MCE

Summary

MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC ₅₀ values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1 , αvβ3 , αvβ5 , αvβ6 , αvβ8 and α5β1 , respectively ^[1] ^[2] ^[3] .

IC50 & Target

αvβ1

1.6 nM (IC ₅₀ , inhibition of fibronectin-binding )

αvβ3

2.8 nM (IC ₅₀ , inhibition of vitronectin-binding)

αvβ5

0.1 nM (IC ₅₀ , inhibition of vitronectin-binding)

αvβ6

0.7 nM (IC ₅₀ , inhibition of LAP-binding)

αvβ8

0.5 nM (IC ₅₀ , inhibition of LAP-binding)

α5β1

12.2 nM (IC ₅₀ , inhibition of fibronectin-binding)

In Vivo

MK-0429 (100 or 300 mg/kg, p.o., twice daily b.i.d., 2 weeks) reduces metastatic tumor colony formation and area in the lungs. MK-0429 is safe and efficacious in significantly decreasing melanoma metastasis in the lungs ^[1] .

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

Animal Model:	B6D2F1 hybrid female mice ^[2]
Dosage:	100 or 300 mg/kg
Administration:	P.o., twice daily (b.i.d.), 2 weeks
Result:	MK-0429 at 100 and 300 mg/kg reduced the number of metastatic tumor colonies by 64 and 57%, respectively, and the high dose also reduced the tumor area by 60% as compared to the vehicle ^[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 : 100 mg/mL ( 227.53 mM ; Need ultrasonic)

H ₂ O : 2.78 mg/mL ( 6.33 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2753 mL	11.3763 mL	22.7526 mL
5 mM	0.4551 mL	2.2753 mL	4.5505 mL
10 mM	0.2275 mL	1.1376 mL	2.2753 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 7.14 mg/mL (16.25 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.62 mg/mL (5.96 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution
4.

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

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution
5.

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

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

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