MK-4101 – 25 mg

Brand:
Cayman
CAS:
935273-79-3
Storage:
-20
UN-No:
Non-Hazardous - /

MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hydroxy steroid dehydrogenase-1. MK-4101 (40 and 80 mg/kg per day) reduces tumor growth in a murine medulloblastoma mouse allograft model, induces tumor regression when administered at a dose of 80 mg/kg twice per day, and reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue.  

 

Available on backorder

SKU: 29159 - 25 mg Category:

Description

A Smoothened receptor antagonist; binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM); inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM); an inhibitor of 11β-hydroxy steroid dehydrogenase-1; reduces tumor growth in a murine medulloblastoma mouse allograft model at 40 and 80 mg/kg per day); induces tumor regression at 80 mg/kg twice per day; reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue


Formal name: 5-(3,3-difluorocyclobutyl)-3-[4-[4-methyl-5-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-3-yl]bicyclo[2.2.2]oct-1-yl]-1,2,4-oxadiazole

Synonyms: 

Molecular weight: 493.5

CAS: 935273-79-3

Purity: ≥98%

Formulation: A crystalline solid