Chemical Structure : LEQ 506
货号: 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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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
分子量 | 432.56 | |
分子式 | C25H32N6O | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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