| CAS NO: | 1261590-48-0 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 416.86 |
|---|---|
| Formula | C22H17ClN6O |
| 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 Name | 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]isoquinolin-1-one |
| Synonyms | IPI145 R-isomer; IPI 145 R enantiomer; IPI-145. INK1197; INK 1197; INK-1197 |
| SMILES | O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)C)=CC5=C1C(Cl)=CC=C5 |
| In Vitro | In 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 Vivo | IPI-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. |
| References | Chem Biol. 2013 Nov 21;20(11):1364-74. |
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