AMG319 - Names and Identifiers
AMG319 - Physico-chemical Properties
Molecular Formula | C21H16FN7
|
Molar Mass | 385.4 |
Density | 1.432±0.06 g/cm3(Predicted) |
Boling Point | 708.3±60.0 °C(Predicted) |
Solubility | DMSO : 40 mg/mL mother liquor preservation: sub-package and freeze storage to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, try to use it now) Cell experiment: Dissolve with DMSO first: dilute with culture medium then, and the dilution process is recommended to be carried out in stages to avoid too fast concentration change leading to compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to avoid excessive concentration changes leading to compound p |
pKa | 9.99±0.10(Predicted) |
Storage Condition | -20℃ |
Use | AMG319 is a potent selective PI3Kδ inhibitor with an IC50 of 18 nM. |
Target | PI3Kα PI3Kβ PI3Kγ PI3Kδ |
In vitro study | AMG 319 inhibited anti-IgM/CD40L-induced B- cell proliferation with an IC50 of 8.6 nM and reduced pAkt levels with an IC50 of 1.5 nM. AMG 319 also inhibited anti-IgD-induced CD-69 expression in HWB. |
In vivo study | In female Lewis rats, AMG 319 (3 mg/kg, p.o.) inhibited the KLH-induced inflammatory response by 88%. In transgenic (IgMm) mice, AMG 319 (, p.o.) inhibited pAKT in vivo with an IC50 of 1.9 nM. |
AMG319 - Reference
Reference Show more | 1. Cushing TD, et al. Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. J Med Chem. 2015 Jan 8;58(1):480-511. |
AMG319 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 2.595 ml | 12.974 ml | 25.947 ml |
5 mM | 0.519 ml | 2.595 ml | 5.189 ml |
10 mM | 0.259 ml | 1.297 ml | 2.595 ml |
5 mM | 0.052 ml | 0.259 ml | 0.519 ml |
Last Update:2024-01-02 23:10:35
AMG319 - Cell Experiment
Cells are seeded in 96-well plates at 2,000 (Sup-T1, Jurkat, and DND-41) or 10,000 (HPB-ALL or TALL-1) cells/well in growth media supplemented with 10% fetal bovine serum. Serial dilutions of Nirogacestat (PF-03084014) are done in DMSO, appropriate controls or designated concentrations of Nirogacestat (PF-03084014) are added to each well, and cells are incubated at 37°C for 7 days (final DMSO content 0.1%). Resazurin at a final concentration of 0.1 mg/mL is added to the cells and plates are incubated for 2 to 4 hours. Fluorescent signals are read as emission at 590 nm after excitation at 560 nm. IC50 values are calculated by using the sigmoidal dose-response (variable slope) in GraphPad Prism.
Last Update:2023-08-16 21:32:38
AMG319 - Animal Experiment
Mice Athymic female mice (nu/nu, 6-8 weeks) are used. For antitumor efficacy, animals bearing tumors of 150 to 300 mm3 in size are randomly divided into groups that received either vehicle (0.5% methylcellulose) or Nirogacestat (PF-03084014) (150 mg/kg, diluted in vehicle), and dosed by oral gavage. Animal body weight and tumor measurements are obtained every 2 to 3 days. Tumor volume (mm3) is measured with Vernier calipers and calculated. Percent (%) inhibition values are measured on the final day of study for drug-treated compared with vehicle-treated mice and are calculated. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used. Student's t test is used to determine the P value.
Last Update:2023-08-16 21:32:38