PKI-179 hydrochloride - ≥98% , CAS No.1463510-35-1

CAS: 1463510-35-1 Cat. No.: P648235 Peso molecular: 525.00 PubChem CID: 137699924

GRADE & PURITY ≥98%

Storage

Store at 2-8°C,Desiccated

Shipped In

Wet ice

Descripción general

PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC 50 s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α , PI3K-β , PI3K-γ , PI3K-δ and mTOR , respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R , with IC 50 s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo

In Vitro

PKI-179 inhibits the cell proliferation, with IC 50 s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively. PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC 50 =3 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors . PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts . PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing MDA-361 human breast cancer tumors Dosage: 5, 10, 25, 50 mg/kg Administration: I.p. every 3 days for 4 weeks Result: Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg. No significant weight loss of tested animals was observed for all different dosages.

Form:Solid

IC50& Target:mTOR 0.42 nM (IC 50 ) PI3Kα 8 nM (IC 50 ) PI3Kβ 24 nM (IC 50 ) PI3Kγ 74 nM (IC 50 ) PI3Kδ 77 nM (IC 50 ) E545K 14 nM (IC 50 ) H1047R 77 nM (IC 50 )

Specifications

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC 50 s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α , PI3K-β , PI3K-γ , PI3K-δ and mTOR , respectively. PKI-179 hydrochloride also exhibits activity over E545K and

Condiciones de almacenamiento de almacenamiento

Store at 2-8°C, Desiccated

Enviado en

Wet ice

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Pureza

≥98%

Nombres e identificadores

• Sonrisas canónicas: C1CC2COCC1N2C3=NC(=NC(=N3)N4CCOCC4)C5=CC=C(C=C5)NC(=O)NC6=CC=NC=C6.Cl
• IUPAC Name: 1-[4-[4-morpholin-4-yl-6-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-1,3,5-triazin-2-yl]phenyl]-3-pyridin-4-ylurea;hydrochloride
• InChIKey: JNMURGIZAFELTR-UHFFFAOYSA-N
• INCHI: 1S/C25H28N8O3.ClH/c34-25(28-19-7-9-26-10-8-19)27-18-3-1-17(2-4-18)22-29-23(32-11-13-35-14-12-32)31-24(30-22)33-20-5-6-21(33)16-36-15-20;/h1-4,7-10,20-21H,5-6,11-16H2,(H2,26,27,28,34);1H
• PubChem CID: 137699924
• Peso molecular: 525.00

Propiedades químicas y físicas

• Solubilidad: DMSO : 20 mg/mL (38.10 mM; Need ultrasonic)