[CAS NO. 1032229-33-6] A939572

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PRODUCTS SPECIFICATIONS [1032229-33-6]

Catelog

HY-50709

Brand

MCE

CAS

1032229-33-6

DESCRIPTION [1032229-33-6]

Overview

MDL	MFCD10698997
Molecular Weight	387.86
Molecular Formula	C20H22ClN3O3
SMILES	O=C(N1CCC(OC2=C(Cl)C=CC=C2)CC1)NC3=CC=CC(C(NC)=O)=C3

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

23 Publications Citing Use of MCE

Summary

A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC ₅₀ values of <4 nM and 37 nM for mSCD1 and hSCD1 , respectively.

IC50 & Target

IC50: <4 nM (mSCD1), 37 nM (hSCD1) ^[1]

In Vitro

A939572 exhibits robust in vivo activity with dose-dependent desaturation index lowering effects ^[1] . A939572 is a small molecule that specifically inhibits SCD1 enzymatic activity. A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5 (IC ₅₀ s of 65 nM, 50 nM, 65 nM, and 6 nM, respectively). In A939572 (SCDi) treated Caki1 and A498 cells, all five ER stress related genes are expressed at significantly increased levels compared to DMSO+BSA control, and this elevated expression can be blocked with the addition of OA-BSA ^[2] .

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

In Vivo

Athymic nude (nu/nu) mice bearing A498 ccRCC xenografts are treated with A939572 (30mg/kg, p.o.) and Tem individually or in combination over the course of four weeks, and tumor volume (mm ³ ) is recorded. A939572 and Tem monotherapy generate similar growth responses with approximately 20-30% reductions in tumor volume (vs. placebo control) being observed upon study completion, with values reaching statistical significance only within the last week of treatment. The combination group yields over a 60% decrease in tumor volume (vs. placebo control) by study completion with significant reductions recorded after approximately 1 week of treatment ^[2] .

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

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 ( 257.82 mM ; Need ultrasonic)

H ₂ O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5782 mL	12.8912 mL	25.7825 mL
5 mM	0.5156 mL	2.5782 mL	5.1565 mL
10 mM	0.2578 mL	1.2891 mL	2.5782 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 (6.45 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

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