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LEQ 506

Chemical Structure : LEQ 506

CAS No.: 1204975-42-7

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LEQ 506 (NPV LEQ 506)

Catalog No.: PC-61758Not For Human Use, Lab Use Only.

LEQ 506 (NPV-LEQ 506) is a second-generation inhibitor of Smoothened (Smo) with IC50 of 2 nM and 4 nM for human and mouse Smo, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LEQ 506 (NPV-LEQ 506) is a second-generation inhibitor of Smoothened (Smo) with IC50 of 2 nM and 4 nM for human and mouse Smo, respectively; also inhibits Smo D473H with IC50 of 96 nM; inhibits Hh signaling in a human cell line, retain activity against a Smo mutant (D473H) cell line; shows efficacy in subcutaneous medulloblastoma models in mice and rats; orally active.

Solid Tumors

Phase 1 Clinical

Physicochemical Properties

M.Wt 432.56
Formula C25H32N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-2-(5-(4-(6-benzyl-4,5-dimethylpyridazin-3-yl)-2-methylpiperazin-1-yl)pyrazin-2-yl)propan-2-ol

References

1. Peukert S, et al. ChemMedChem. 2013 Aug;8(8):1261-5.

2. Lauressergues E, et al. Pharmacol Res Perspect. 2016 Mar 4;4(2):e00214.

3. Tu J, et al. Pharmacol Res. 2017 Nov 21. pii: S1043-6618(17)31322-1.

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