[CAS NO. 287405-51-0] Apratastat

Name: Apratastat
Brand: Arctom Scientific
SKU: AS950837

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PRODUCTS SPECIFICATIONS [287405-51-0]

Distributor

Catalog

AS950837

Brand

Arctom Scientific

CAS

287405-51-0

DESCRIPTION [287405-51-0]

Overview

MDL	MFCD13152357
Molecular Weight	414.50
Molecular Formula	C17H22N2O6S2
SMILES	CC1(C)[C@H](C(NO)=O)N(S(=O)(C2=CC=C(OCC#CCO)C=C2)=O)CCS1

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

Summary

Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α . Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) ^[1] ^[2] .

IC50 & Target

MMP

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00095342	Wyeth is now a wholly owned subsidiary of Pfizer	Rheumatoid Arthritis		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 : 41.4 mg/mL ( 99.88 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4125 mL	12.0627 mL	24.1255 mL
5 mM	0.4825 mL	2.4125 mL	4.8251 mL
10 mM	0.2413 mL	1.2063 mL	2.4125 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 (6.03 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

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