A substituted diarylimidazole inhibitor of P-glycoprotein ATPase activity (IC50 = 0.16 µM); reverses drug resistance to doxorubicin

ONT-093 – 1 mg

Brand:
Cayman
CAS:
216227-54-2
Storage:
-20
UN-No:
Non-Hazardous - /

ONT-093 is an orally bioavailable substituted diarylimidazole inhibitor of P-glycoprotein ATPase activity (IC50 = 0.16 µM).{48625} It reverses drug resistance to doxorubicin (Item No. 15007), vinblastine (Item No. 11762), and paclitaxel (Item No. 10461) in human lymphoma, breast, ovarian, uterine, and colorectal cancer cell lines in vitro (EC50s = 9-38 nM). It is not cytotoxic to 15 normal, non-transformed, or tumor cell lines when used at concentrations up to 100 µM and exhibits weak cytostatic activity (average IC50 = >60 µM). ONT-093 (30 mg/kg) reverses paclitaxel drug resistance in an HCT15 human colon carcinoma mouse xenograft model.  

 

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SKU: 28758 - 1 mg Category:

Description

A substituted diarylimidazole inhibitor of P-glycoprotein ATPase activity (IC50 = 0.16 µM); reverses drug resistance to doxorubicin, vinblastine, and paclitaxel in human lymphoma, breast, ovarian, uterine, and colorectal cancer cell lines (EC50s = 9-38 nM); not cytotoxic at concentrations up to 100 µM; exhibits weak cytostatic activity (average IC50 = >60 µM); reduces paclitaxel drug resistance in an HCT15 human colon carcinoma mouse xenograft model at 30 mg/kg

Formal name: 4-[2-[4-[(1E)-3-ethoxy-1-propen-1-yl]phenyl]-4-[4-[(1-methylethyl)amino]phenyl]-1H-imidazol-5-yl]-N-(1-methylethyl)-benzenamine

Synonyms:  OC 144093

Molecular weight: 494.7

CAS: 216227-54-2

Purity: ≥98%

Formulation: A crystalline solid

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