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Chemdea |
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PKI-179 – PI3Ka/mTOR
Inhibitor |
Catalog # CD0296 |
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Price: 1 mg - $99;
5 mg - $150; 10 mg - $250; 25 mg - $550; 50 mg - $990; 100 mg - $1750 |
Availability: Inquire |
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N-[4-[4-(4-Morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl]phenyl]-N'-4-pyridinylurea
hydrochloride
White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 97% by HPLC. CAS# 1197160-28-3. Solubility: DMSO (35 mg/mL). The hydrochloride form shows improved solubility as compared to the free base form. Molecular Formula: C25H28N8O3*HCl. Molecular Weight: 525.00.
PKI-179 is an orally efficacious dual PI3K/mTOR inhibitor. PKI-197 potently inhibited in in vitro enzymatic assay PI3Ka, PI3Kg and mTORC1/mTORC2 (IC50 = 8 mM, 74 nM and 0.42 nM respectively) and it showed significant activity against MDA-361 and PC3mm2 cell lines (IC50 = 22 mM, 29 nM respectively). PKI-179 showed excellent selectivity against 361-membered kinase panel (IC50 > 50 mM). Pharmacokinetic studies of PKI-197 showed good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey and 61% in dog) and high half-life (>60 min). Evaluation of in vivo efficacy in nude mouse model bearing MDA-361 human breast cancer tumors showed pronounced tumor growth arrest when dosed above 10 mg/Kg.
References: Venkatesan, A. M., et al. Bioorg. Med. Chem. Lett. 2010, 20, 5869. |
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CHEMDEA; |