PI3Kδ-IN-1 - 10mM in DMSO , CAS No.1911564-39-0

CAS: 1911564-39-0 Cat. No.: P656805 Summenformel: C₂₂H₂₀F₃N₇O₂ Molekulargewicht: 471.44 PubChem CID: 132220479

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC 50 of 1.7 nM.

In Vitro

PI3Kδ-IN-1 (compound 52) shows >100-fold selectivity over the other PI3K isoforms. Kinome selectivity is also excellent with >660-fold selectivity over MNK1 and others in HTRF assays. Importantly, PI3Kδ-IN-1 has an improved human/rodent in vitro stability correlation and a good permeability profile. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PI3Kδ-IN-1 (2, 5 mg/kg, orally b.i.d. for 42 days) shows greater than 50% suppression of paw swelling in mice. PI3Kδ-IN-1 has an EC 50 of 10 nM at 24 h ( ED 50 of ∼1.25 mg/kg) in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male DBA/1 mice (20−25g) Dosage: 0.5, 2, 5 mg/kg Administration: Oral b.i.d. for 42 days, Result: A dose dependent reduction of the clinical score was observed. Doses of 2 and 5 mg/kg showed greater than 50% suppression of paw swelling .

IC50& Target:IC50: 1.7 nM (PI3Kδ)

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC 50 of 1.7 nM.

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

• Isomere SMILES: CC(=O)N1CCN(C(=O)C1(C)C)C2=C(C=CC(=C2)C3=CC(=C4N3N=CN=C4N)C(F)(F)F)C#N
• PubChem CID: 132220479
• Molekulargewicht: 471.44

Zugehörige Ziele (menschlich)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (0 Activities)

Discover Target: PIK3CG

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

PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (0 Activities)

Discover Target: PIK3CA

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

PIK3CD Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (0 Activities)

Discover Target: PIK3CD

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

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.

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

The CAS Number is 1911564-39-0, the molecular formula is C22H20F3N7O2, and the molecular weight is 471.44 g/mol.

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 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.