PI3Kα-IN-4 - 10mM in DMSO , CAS No.2322293-83-2

CAS: 2322293-83-2 Cat. No.: P655052 Summenformel: C₂₅H₂₃ClFN₅O₅S Molekulargewicht: 560.00

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα , with an IC 50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity

In Vitro

PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC 50 s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays. PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC 50 s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit tumor growth by 73.0% in mice . PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily for 30 d) dose dependently suppresses tumor growth by 62.5% (15 mg/kg), 86.0% (30 mg/kg) and 90.7% (40 mg/kg), respectively in mice . PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily; 1-4 h) inhibits the phosphorylation of Akt in a dose- and time-dependent manner in vivo . PI3Kα-IN-4 shows high C max (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) following oral administration (mouse 10, rat 3 mg/kg) . PI3Kα-IN-4 shows t 1/2 (mouse 0.99, rat 1.22 h) and low plasma clearance (mouse 4.16, rat 5.28 mL/min/kg) following intravenous injection (mouse 1, rat 1 mg/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BT-474 subcutaneous xenograft mice Dosage: 30 mg/kg Administration: P.o. once daily for 21 days Result: Inhibited tumor growth by 73.0% and could be tolerated.

IC50& Target:PI3Kα 1.8 nM (IC 50 )

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα , with an IC 50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Namen und Kennungen

• Molekulargewicht: 560.00

Häufig gestellte Fragen

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2322293-83-2, the molecular formula is C25H23ClFN5O5S, and the molecular weight is 560.00 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.