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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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D409210-1ml | 1ml | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $330.90 |
p110β Selective Inhibitors
Specifications & Purity | Moligand™, 10mM in DMSO |
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Biochemical and Physiological Mechanisms | Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. |
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | Information Duvelisib (IPI-145, INK1197) is a novel and selectivePI3K δ/γinhibitor withKiandIC50of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. 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 ng•h/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. cell lines:H1299, HCT116, DU145, PC3 and MDA435 cells Concentrations: Incubation Time: Powder Purity:≥99% |
Ki Data | PI3Kβ, Ki: 1564 pM |
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Canonical SMILES | CC(NC1=NC=NC2=C1N=C[NH]2)C3=CC4=CC=CC(=C4C(=O)N3C5=CC=CC=C5)Cl |
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Molecular Weight | 416.86 |
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Solubility | Solubility (25°C) In vitro DMSO: 11 mg/mL (23.94 mM); Water: Insoluble; Ethanol: Insoluble; |
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