Antibodies
IPI-145 (INK1197)
- 貨號 Cat. No.
- S7028
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
IPI-145 (INK1197)
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, highly selective for PI3K δ/γ than other protein kinases. Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | 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, highly selective for PI3K δ/γ than other protein kinases. Phase 2. | |||||
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| Targets | PI3K δ | PI3K γ | ||||
| IC50 | 23 pM (Ki)/1 nM (IC50) | 243 pM (Ki)/50 nM (IC50) [1] | ||||
| In vitro | 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. [1] | |||||
| 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. [1] | |||||
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Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01476657 | Recruiting | Hematologic Malignancies | Infinity Pharmaceuticals, Inc. | 2011-10 | Phase 1 |
| NCT01653756 | Recruiting | Asthma | Infinity Pharmaceuticals, Inc. | 2012-07 | Phase 2 |
| NCT01836861 | Completed | Healthy | Infinity Pharmaceuticals, Inc. | 2013-03 | Phase 1 |
| NCT01851707 | Recruiting | Rheumatoid Arthritis | Infinity Pharmaceuticals, Inc. | 2013-04 | Phase 2 |
| NCT01871675 | Recruiting | Lymphoma|Chronic Lymphocytic Leukemia|Non-Hodgkin Lymphoma|T-cell Lymphoma | Sarah Cannon Research Institute|Infinity Pharmaceuticals, Inc. | 2013-05 | Phase 1 |
Chemical Information
Download IPI-145 (INK1197) SDF
| Molecular Weight (MW) | 416.86 |
|---|---|
| Formula | C22H17ClN6O |
| CAS No. | 1201438-56-3 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 84 mg/mL (201 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 1(2H)-Isoquinolinone, 8-chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.41686 | 4.1686 | 8.3372 | 12.5058 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | Dr Antonino Maria Spartà from University of Bologna. IPI-145 (INK1197) purchased from Selleck | |
| Method | MTT | |
| Cell Lines | ALL-SIL cells | |
| Concentrations | ||
| Incubation Time | 48 h | |
| Results | PI3K inhibitor IPI-145 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range. |
