PF-06843195 - 10mM in DMSO , CAS No.2067281-51-8

CAS: 2067281-51-8 Cat. No.: P656841 Fórmula: C₂₀H₂₅F₃N₈O₄ Peso molecular: 498.46 PubChem CID: 124193915

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

PF-06843195 is a highly selective PI3Kα inhibitor with an IC 50 of 18 nM in Rat1 fibroblasts. The K i s of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy

In Vitro

PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC 50 s of 62 nM and 32 nM, respectively. PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC 50 s of 7.8 nM and 8.7 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309 . PF-06843195 exhibits oral bioavailability (rat 25 %) following oral administration (rat 10 mg/kg) . PF-06843195 exhibits a moderate half-life (rat 3.6 h) due to high plasma clearance (30 mL/min/kg) combined with large volumes of distribution (3.0 L/kg) following intravenous administration (rat 2 mg/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar Han Rats Dosage: 2 mg/kg (intravenous) and 10 mg/kg (oral gavage)(Pharmacokinetic Analysis) Administration: Intravenous (IV) or oral gavage (PO) Result: T 1/2 of 3.6 h for rats.

IC50& Target:PI3Kα 18 nM (IC 50 , in Rat1 fibroblasts) PI3Kβ 360 nM (IC 50 , in Rat1 fibroblasts) PI3Kδ 160 nM (IC 50 , in Rat1 fibroblasts) PI3Kα 0.018 nM (Ki) PI3Kδ 0.28 nM (Ki)

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

PF-06843195 is a highly selective PI3Kα inhibitor with an IC 50 of 18 nM in Rat1 fibroblasts. The K i s of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of t

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: C1CN(C[C@@]1(CO)NC2=NC(=NC(=C2F)C3=CN=C(N=C3)N)N4CCOCC4)C(=O)OCC(F)F
• CAS alternativo: 2067281-51-8
• PubChem CID: 124193915
• Peso molecular: 498.46

Objetivos asociados (humanos)

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (1 Activities)

Discover Target: PIK3CA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Preguntas frecuentes

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 2067281-51-8, the molecular formula is C20H25F3N8O4, and the molecular weight is 498.46 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.