- Duvelisib (IPI-145; INK1197)
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- $15.00 / 1KG
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2021-07-13
- CAS:1201438-56-3
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- Duvelisib (IPI-145; INK1197)
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- $15.00 / 1KG
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2021-07-10
- CAS:1201438-56-3
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- IPI 145
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- $5.00 / 5KG
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2019-09-04
- CAS:1201438-56-3
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 1ton
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| IPI 145 Basic information |
Product Name: | IPI 145 | Synonyms: | IPI-145;IPI-145 (INK-1197);IPI-145 INK197;8-Chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone;IPI-145, >=98%;Duvelisib (IPI-145, INK1197);DUVELISIB (IPI-145);1(2H)-Isoquinolinone, 8-chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]- | CAS: | 1201438-56-3 | MF: | C22H17ClN6O | MW: | 416.86 | EINECS: | 200-256-5 | Product Categories: | reference inhibitors;Inhibitors | Mol File: | 1201438-56-3.mol | ![IPI 145 Structure](CAS/GIF/1201438-56-3.gif) |
| IPI 145 Chemical Properties |
Melting point | 205-206o C | Boiling point | 757.8±60.0 °C(Predicted) | density | 1.474±0.06 g/cm3(Predicted) | storage temp. | -20°C | solubility | Soluble in DMSO (up to at least 25 mg/ml) | form | White solid. | pka | 10.05±0.10(Predicted) | color | White | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| IPI 145 Usage And Synthesis |
Description | Duvelisib (1201438-56-3) is a potent and selective (IC50’s: PI3Kα = 1602nM, PI3Kβ = 85nM, PI3Kδ= 2.5nM, PI3Kγ = 27nM) dual PI3Kδ/γ inhibitor.1 It inhibits B and T cell proliferation, blocks neutrophil migration, and inhibits basophil activation. Duvelisib antagonizes B-cell receptor cross-linking activated pro-survival signals in primary chronic lymphocytic leukemia cells.2?Duvelisib also shows preclinical/clinical activity against other hematologic malignancies such as Non-Hodgkins lymphoma, T-cell lymphoma, and others.3,4?Useful clinical agent for the treatment of various blood cancers. Low-dose treatment of T-cell-inflamed tumor models of head and neck cancers with Duvelisib enhanced responses to PD-L1 blockade via suppression of myeloid-derived suppressor cells.5?Higher doses reversed the effect due to suppression of tumor-infiltrating T lymphocytes | Uses | IPI 145 is an 1,2-dihydroisoquinolin-1(2H)-one derivative and has been developed as a modulator of PI3 kinase. | Definition | ChEBI: 8-chloro-2-phenyl-3-[(1S)-1-(7H-purin-6-ylamino)ethyl]-1-isoquinolinone is a member of isoquinolines. | Brand name | Copiktra | General Description | Class: lipid kinase;
Treatment: CLL, SLL, FL;
Other name: INK1197, IPI145;
Oral bioavailability = 42%;
Elimination half-life = 4.7 h;
Protein binding = 98% | Pharmacokinetics | The recommended dose of duvelisib is 25 mg
twice daily, much lower than that of idelalisib (150 mg,
bid). Duvelisib is rapidly absorbed, with a peak
concentration after 1–2 h. Following the
administration of 25 mg of duvelisib, the absolute
bioavailability in healthy volunteers is 42%. It is
eliminated with a short half-life of 4.7 h, thus
requiring twice daily administration. | target | PI3Kγ/δ | IC 50 | ![IC 50 of IPI 145 IC 50 of IPI 145](/NewsImg/2024-05-22/6385198760949493187529534.png) | Metabolism | Duvelisib is
primarily metabolized by CYP3A4 to give a monooxidation product, IPI-656, which has no
pharmacologically relevant activity.
![Metabolic pathway of duvelisib in humans Metabolic pathway of duvelisib in humans](/NewsImg/2024-05-22/6385198800289519809549322.png) | References | 1) Winkler?et al.?(2013),?PI3K-δ and PI3K-γ Inhibition by IPI-145 Abrogates Immune Response and Suppresses Activity in Autoimmune and Inflammatory Disease Models;?Chem. Biol.?20?1309
2) Dong?et al.?(2014),?IPI-145 antagonizes intrinsic and extrinsic survival signals in chronic lymphocytic leukemia cells;?Blood?124?3583
3) Flinn?et al.?(2018),?Duvelisib, a novel dual inhibitor of PI3K-δ/γ, is clinically active in advances hematologic malignancies;?Blood?131?877
4) Faia?et al.?(2018),?The phosphoinositide-3 kinase (PI3K)-δ,γ inhibitor, duvelisib, shows preclinical synergy with multiple targeted therapies in hematologic malignancies;?PLoS One?13?e0200725
5) Davis?et al.?(2017),?Anti-PD-L1 Efficacy Can Be Enhanced by Inhibition of Myeloid-Derived Suppressor Cells with a Selective Inhibitor of PI3Kδ/γ;?Cancer Res.?77?2607 |
| IPI 145 Preparation Products And Raw materials |
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