Antibodies
LY3039478 is a novel and orally bioavailable inhibitor of Notch-1 intracellular domain (N1ICD) cleavage with IC50 of ~1 nM. Phase 1.
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| Description | LY3039478 is a novel and orally bioavailable inhibitor of Notch-1 intracellular domain (N1ICD) cleavage withIC50 of ~1 nM. Phase 1. | |||||
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| Targets | Notch-1 | |||||
| IC50 | ~1 nM [1] | |||||
| In vitro | LY3039478 potently inhibits mutant Notch receptor activity in vitro. [1] | |||||
| In vivo | In vivo, LY3039478 inhibits N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment, which results in the induction of apoptosis in a Notch-dependent xenograft model.[1] | |||||
| Features | ||||||
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
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| NCT01695005 | Recruiting | Neoplasms|Neoplasm Metastasis|Lymphoma | Eli Lilly and Company | 2012-10 | Phase 1 |
| Molecular Weight (MW) | 464.44 |
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| Formula | C22H23F3N4O4 |
| CAS No. | 1421438-81-4 |
| 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 | Butanamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-(2-hydroxyethyl)-6-oxo-5H-pyrido[3,2-a][3]benzazepin-7-yl]amino]-1-methyl-2-oxoethyl]-4,4,4-trifluoro- |
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