AZD2014 Inhibitor CAS No. 1009298-59-2

Cat. No.	Name	Size	Price
KI1131	AZD2014	5 mg	$232
	AZD2014	10 mg	$330
	AZD2014	25 mg	$660
	AZD2014	50 mg	$930

Chemical Characteristic

Product Name	AZD2014
CAS No.	1009298-59-2
Molecular Weight	462.54
Formula	C₂₅H₃₀N₆O₃
Chemical Name	3-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]pyrimidin-7-yl]-N-methylbenzamide
Smiles	C(=O)(c1cc(ccc1)c1ccc2c(nc(nc2n1)N1[C@H](COCC1)C)N1[C@H](COCC1)C)NC
Chemical Structure

Biological activities

AZD2014 is a mammalian target of rapamycin (mTOR) C1/C2 dual inhibitor. Exposure of GSCs to AZD2014 for 1 hour results in complete inhibition of mTORC1 and 2 activities. AZD2014 treatment inhibits the repair of radiation induced double strand breaks (DSBs). Addition of AZD2014 1 hour before irradiation enhances the radiosensitivity of three GSC cell lines. ^[1] AZD2014 decreases p4EBP1 Thr37/46, inhibits the translation initiation complex and decreases overall protein synthesis. AZD2014 also inhibits the mTORC2 biomarkers pAKTSer473 and pNDRG1Thr346, and has broad antiproliferative activity across multiple tumor cell lines. Besides, AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER⁺ cell lines with acquired resistance to hormone therapy. In vivo, AZD2014 induces tumor growth inhibition against several xenograft models including a human primary explant model of ER⁺ breast cancer refractory to tamoxifen. ^[2]

References

[1] Kahn J, et al. The mtorc1/mtorc2 inhibitor azd2014 enhances the radiosensitivity of glioblastoma stem-like cells. International Journal of Radiation Oncology Biology Physics. 2012, 84(3), Supplement 1: S697. [2] Guichard Sylvie M., et al. AZD2014, a dual mTORC1 and mTORC2 inhibitor is differentiated from allosteric inhibitors of mTORC1 in ER+ breast cancer. Cancer Research. 2012, 72(8): abstract 917.

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