Antibodies
AZD2014
- 貨號 Cat. No.
- S2783
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
AZD2014
AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM; highly selective against multiple PI3K isoforms (α/β/γ/δ). Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | AZD2014 is a novel mTOR inhibitor with IC50 of 2.8 nM; highly selective against multiple PI3K isoforms (α/β/γ/δ). Phase 2. | |||||
|---|---|---|---|---|---|---|
| Targets | mTOR | |||||
| IC50 | 2.8 nM [1] | |||||
| In vitro | AZD2014 is a close analogue of AZD8055 and a selective inhibitor of mTOR kinase. AZD2014 has greater inhibitory activity against mTORC1 compared to rapamycin: AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis while rapamycin has no effect. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. In particular, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy. [1] | |||||
| In vivo | AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen. The antitumour activity is associated with modulation of both mTORC1 and mTORC2 substrates. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01026402 | Recruiting | Advanced Solid Malignancies | AstraZeneca | 2009-12 | Phase 1 |
| NCT01597388 | Recruiting | Advanced Metastatic Breast Cancer | AstraZeneca | 2012-05 | Phase 1 |
| NCT01793636 | Recruiting | Metastatic Clear Cell Renal Carcinoma | Queen Mary University of London|AstraZeneca|Cancer Research UK | 2013-02 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 462.54 |
|---|---|
| Formula | C25H30N6O3 |
| CAS No. | 1009298-59-2 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 38 mg/mL (82 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 | 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.46254 | 4.6254 | 9.2508 | 13.8762 |
Customer Reviews (4)
 Click to enlarge | Rating | |
| Source | Dr Milica Pesic from Institute for Biological Research.AZD2014 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | NCI-H460 cells /NCI-H460/R cells | |
| Concentrations | 100/250 nM | |
| Incubation Time | 18 h | |
| Results | Concentration-dependent cell growth inhibition induced by AZD2014 did not differ between sensitive (NCI-H460) and multi-drug resistant (NCI-H460/R) human non-small cell lung carcinoma cell lines (A). AZD2014 cell growth inhibition efficacy decreased in multi-drug resistant colorectal carcinoma cell line DLD1-TxR in comparison to its sensitive counterpart DLD1 (B). The results were obtained by the Sulforhodamine B assay. All values represent average ?SD obtained from two independent experiments, n = 5. (DLD1 possesses mutated p53, while its resistant counterpart DLD1-TxR additionally acquired the LOH in PTEN gene during the course of resistance induction.) |
Product Citations (3)
Rapamycin Induces MAP Kinase Phosphatase (MKP)-1 Expression Through Activation of Protein Kinase B and Mitogen-activated Protein Kinase Kinase Pathways. [Rastogi R, et al. J Biol Chem 2013;288(47):33966-77]
PubMed: 24126911
The dual mTORC1 and mTORC2 inhibitor AZD8055 inhibits head and neck squamous cell carcinoma cell growth in vivo and in vitro [Li Q,et al. Biochem Biophys Res Commun 2013;440(4):701-6]
PubMed: 24103749
Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. [Huo HZ, et al. Biochem Biophys Res Commun 2013;443(2):406-12]
PubMed: 24309100
