1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)

A939572 (Synonyms: stearoyl-CoA desaturase (SCD) inhibitor; SCD-inhibitor; 1-Piperidinecarboxamide, 4-(2-chlorophenoxy)-N-[3-[(methylamino)carbonyl]phenyl]-)

Cat. No.: HY-50709 Purity: 99.79%
Data Sheet SDS Handling Instructions

A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.

For research use only. We do not sell to patients.
A939572 Chemical Structure

A939572 Chemical Structure

CAS No. : 1032229-33-6

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Free sample   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
2 mg $60 In-stock
5 mg $90 In-stock
10 mg $120 In-stock
50 mg $480 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 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 (IC50s 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].

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 (mm3) 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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[2]

A939572 is dissolved in DMSO and stored, and then diluted with appropriate media before use[2].

Cells are plated (0.5 or 1×105/well) in 24-well plates in triplicate. Cells are counted using a Coulter Particle Counter. Oleic acid-albumin is added to media at 5μMol. A939572 stocks are prepared in DMSO. Temsirolimus dosing is performed. Soft agar cultures are prepared by diluting 2× growth medium 1:1 in 1.5% Seaplaque®GTG® agarose, with 500 cells/plate in 60mm culture dishes. Colonies are stained with Giemsa and counted after 3wks[2].

Animal Administration
[2]

A939572 is re-suspended in strawberry flavored Kool-Aid® in sterilized H2O (Mice)[2].

Mice[2]
A498 cells are subcutaneously implanted in athymic nu/nu mice at 1×106 cells/mouse in 50% Matrigel. Tumors reach ~50 mm3 prior to 4 wk treatment. A939572 is re-suspended in strawberry flavored Kool-Aid® in sterilized H2O (0.2 g/mL) vehicle at 30 mg/kg in a 50 μL dose. Mice are orally fed by using a syringe to administer the 50 μL dose twice daily/mouse. This modified method is found to be effective and less stressful on the mice. Temsirolimus is solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10 mg/kg in a 50 μL dose once every 72 hrs/mouse. Tumor volumes are calculated using the formula 0.5236 (L*W*H) and body weight are measured every 3 days.

References
M.Wt

387.86

Formula

C₂₀H₂₂ClN₃O₃

CAS No.

1032229-33-6

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 56 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
A939572
Cat. No.:
HY-50709
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