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Vistusertib (AZD2014)

Vistusertib (AZD2014)

Item no.	S2783-5
Manufacturer	Selleckchem
CASRN	1009298-59-2
Amount	5 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 5 mg 5 g
Category	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer
Type	Inhibitors
Specific against	other
Smiles	CC1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=CC=C4)C(=O)NC)N5CCOCC5C
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1009298-59-2'
Similar products	AZD2014
Available
Manufacturer - Targets	MTOR
Storage Conditions	2 years -80 in solvent
Molecular Weight	462, 54
Clinical Trials	AZD2014 is now under Phase 1 clinical trial to assess the safety, tolerability, pharmacokinetics and preliminary efficacy in advanced solid malignancies.
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]
Solubility (25C)	DMSO 38 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Vistusertib (AZD2014) is a novel mTOR inhibitor with IC50 of 2.8 nM in a cell-free assay; highly selective against multiple PI3K isoforms (α/β/γ/δ). AZD2014 showed no or weak binding to the majority of kinases when tested at 1 μM. AZD2014 induces proliferation suppression, apoptosis, cell cycle arrest, and autophagy in HCC cells with antitumor activity.
Chemical Name	3-(2, 4-bis((S)-3-methylmorpholino)pyrido[2, 3-d]pyrimidin-7-yl)-N-methylbenzamide

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S2783-5-datasheet.pdf

S2783-5-safety-datasheet.pdf