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Duvelisib R enantiomer
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Duvelisib R enantiomer图片
CAS NO:1261590-48-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)416.86
FormulaC22H17ClN6O
CAS No.1261590-48-0 (R-isomer);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 83 mg/mL (199.1 mM)
Water:<1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo) 30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL
Chemical Name8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one
SynonymsIPI145 R-isomer; IPI 145 R enantiomer; IPI-145. INK1197; INK 1197; INK-1197
SMILESO=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)C)=CC5=C1C(Cl)=CC=C5
实验参考方法
In VitroIn Vitro Assay: Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively. PI3Kδ and PI3Kγ inhibition with IPI-145 has anti-proliferative activity in primary AML cells by inhibiting the activity of AKT and MAPK. Pre-treatment of AML cells with IPI-145 inhibits both adhesion and migration of AML blasts to bone marrow stromal cells

Cell Assay: IPI-145 suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM.

In VivoIPI-145 (10 mg/kg, p.o.) shows well pharmacokinetics with Cmax and AUC of 390 ng/mL and 137 ngoh/mL in mouse and rat. IPI-145 (10 mg/kg) is active in murine DTH model with ~50% ear swelling. IPI-145 (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model. IPI-145 prevents inflammation and protects joint bone and cartilage in the rat CIA model. IPI-145 (10 mg/kg,QD) demonstrates activity in rat adjuvant induced polyarthritis model.
Animal model Mouse and rat with collagen induced arthritis (CIA) model.
Formulation & Dosage 10 mg/kg, p.o.
ReferencesChem Biol. 2013 Nov 21;20(11):1364-74.