GNE-272 - Moligand™,10mM in DMSO , CAS No.1936428-93-1

CAS: 1936428-93-1 Cat. No.: G655063 Summenformel: C₂₂H₂₅FN₆O₂ Molekulargewicht: 424.47 PubChem CID: 121372887

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC 50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4 , respectively. GNE-272 is also a selective in vivo probe for CBP/EP300

In Vitro

GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC 50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound C max of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4)

Specifications

Spezifikationen & Reinheit

Moligand™,10mM in DMSO

Biochemische und physiologische Mechanismen

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC 50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4 , respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

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

Note

Moligand™

Aktionsart

INHIBITOR

Namen und Kennungen

• Isomere SMILES: CC(=O)N1CCC2=C(C1)C(=NN2[C@H]3CCOC3)NC4=C(C=C(C=C4)C5=CN(N=C5)C)F
• PubChem CID: 121372887
• Molekulargewicht: 424.47

Zugehörige Ziele (menschlich)

CREBBP Tchem CREB-binding protein (3 Activities)

Discover Target: CREBBP

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

Häufig gestellte Fragen

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

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 1936428-93-1, the molecular formula is C22H25FN6O2, and the molecular weight is 424.47 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.