Antibodies
LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2.
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| Description | LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2. | |||||
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| Targets | GSK-3α | GSK-3β | ||||
| IC50 | 1.5 nM | 0.9 nM [1] | ||||
| In vitro | LY2090314 selectively inhibits the activity of GSK-3 by interrupting ATP binding. LY2090314 is able to stabilize β-catenin. LY2090314 shows limited efficacy as monotherapy. LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer cell lines in vitro. [1] | |||||
| In vivo | LY3090314 enhances the efficacy of cisplatin and carboplatin in solid tumor cancer xenografts. [1] | |||||
| Features | ||||||
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01287520 | Completed | Advanced Cancer | Eli Lilly and Company | 2007-11 | Phase 1 |
| NCT01214603 | Completed | Leukemia | Eli Lilly and Company | 2010-11 | Phase 2 |
| NCT01632306 | Recruiting | Pancreatic Cancer | Eli Lilly and Company|Mayo Clinic | 2013-03 | Phase 1|Phase 2 |
| Molecular Weight (MW) | 512.53 |
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| Formula | C28H25FN6O3 |
| CAS No. | 603288-22-8 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
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| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <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 | 3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-4-(imidazo[1,2-a]pyridin-3-yl)-1H-pyrrole-2,5-dione |
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