Roginolisib - 10mM in DMSO , CAS No.1305267-37-1

CAS: 1305267-37-1 Cat. No.: R655604 Molecular Weight: 526.58 PubChem CID: 66580799

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC 50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases

In Vitro

Roginolisib (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC 50 values of 280?nM. Roginolisib inhibits B cell proliferation in a concentration-dependent manner with an IC 50 of 48?nM. Roginolisib blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: B cells Concentration: 0-10 μM Incubation Time: 1 hour Result: Inhibited B cell proliferation in a concentration-dependent manner with an IC 50 of 48 nM.

In Vivo

Roginolisib (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NZB/W F1 female mice Dosage: 6.6, 22, or 66 mg/kg Administration: Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10 weeks Result: Significantly reduced proteinuria incidence and severity in a dose-dependent manner.

IC50& Target:PI3Kδ 145 nM (IC 50 ) PI3Kα 18500 nM (IC 50 ) PI3Kβ 2850 nM (IC 50 )

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC 50 of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: C1COCCN1CC2=CC=C(C=C2)N3C4=C(CS(=O)(=O)C5=C4C=CC=C5F)C(=N3)C(=O)N6CCOCC6
• Alternate CAS: 1305267-37-1
• PubChem CID: 66580799
• Molecular Weight: 526.58