Liarozole (R 75251, R75,251) is an orally active benzimidazole-based retinoic acid (RA) metabolism blocking agent (RAMBA) that targets multiple P450 enzymes, including aromatase (CYP19), 17-hydroxylase/17,20-lyase (CYP17A1), 11-hydroxylase (CYP11B1), and RA 4-hydroxylase (CYP26). Liarozole is more effective than ketoconazole in vivo (plasma RA enhancement = 2.5 ng/mL vs. 1.3 ng/mL 2 hr after respective oral dosage of 40 mg/kg in rats) and, in contrast to ketoconazole, Liarozole does not significantly affect circulating adrenal androgen levels. Liarozole is shown to effectively suppress androgen-dependent tumor expansion of R3327G Dunning prostate adenocarcinoma xenografts in rats (by 66% and 81% with 80 and 120 mg/kg/day p.o., respectively) independent of its androgen biosynthesis inhibition.
| Molecular Weight | 381.69 |
| Formula | C17H13ClN4 · 2HCl |
| CAS Number | 1883548-96-6 |
| Solubility (25°C) | Water: 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Products |
|---|
| Izeltabart
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C to synthesize IMGC936, an Antibody-drug Conjugate with strong anti-cancer activity. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models. |
| Cofetuzumab
Cofetuzumab (PF-06523435) is a humanized IgG1-κ monoclonal antibody targeting PTK7. |
| Crizanlizumab
Crizanlizumab is an anti-P-selectin monoclonal antibody. Crizanlizumab binds to P-selectin and blocks its interaction with P-selectin glycoprotein ligand 1 (PSGL-1). Crizanlizumab prevents vaso-occlusive crises (VOCs). |
| M3554 (anti-GD2 ADC)
M3554 is a novel anti-GD2 ADC designed based on humanized ch14.18 anti-GD2 antibody. M3554 has anti-tumor activity. |
| OGT2115
OGT2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT2115 has anti-angiogenic properties (IC50 = 1 μM). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
