Antibodies
BYL719
- 貨號 Cat. No.
- S2814
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
BYL719
BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. Phase 1/2.
| Size | Price | Stock | Quantity | ||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||||||||||||||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. Phase 1/2. | |||||
|---|---|---|---|---|---|---|
| Targets | PI3Kα | |||||
| IC50 | 5 nM [1] | |||||
| In vitro | BYL719 inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway. [1] | |||||
| In vivo | BYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. BYL719(270mg/d) shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01735968 | Recruiting | 3rd Line GIST | Novartis|Novartis Pharmaceuticals | 2013-02 | Phase 1 |
| NCT01791478 | Recruiting | Estrogen Receptor-positive Breast Cancer|HER2-negative Breast Cancer|Invasive Ductal Breast Carcinoma|Progesterone Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer | Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) | 2013-04 | Phase 1 |
| NCT01870505 | Recruiting | Metastatic or Locally-advanced Unresectable Breast Cancer | Memorial Sloan-Kettering Cancer Center|Novartis Pharmaceuticals | 2013-05 | Phase 1 |
| NCT01822613 | Not yet recruiting | Esophageal Squamous Cell Carcinoma | Novartis|Novartis Pharmaceuticals | 2013-06 | Phase 1|Phase 2 |
| NCT01872260 | Not yet recruiting | Breast Cancer | Novartis|Novartis Pharmaceuticals | 2013-07 | Phase 1|Phase 2 |
Chemical Information
| Molecular Weight (MW) | 441.47 |
|---|---|
| Formula | C19H22F3N5O2S |
| CAS No. | 1217486-61-7 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 88 mg/mL (199 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 2 mg/mL (4 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 | 1,2-Pyrrolidinedicarboxamide, N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-, (2S)- |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.44147 | 4.4147 | 8.8294 | 13.2441 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | BYL719 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | A549 cells | |
| Concentrations | 1-20 uM | |
| Incubation Time | 24 h | |
| Results | This PI3K inhibitor dramatically reduced AKT phosphorylation at 10uM. Downstream Cyclin D1 phosphorylation were also inhibited. |
Product Citations (1)
PI3KCA plays a major role in multiple myeloma and its inhibition with BYL719 decreases proliferation, synergizes with other therapies and overcomes stroma-induced resistance. [Azab F, et al. Br J Haematol 2013;10.1111/bjh.12734]
PubMed: 24405121
