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AZD2014

Cat. No. M2299
AZD2014 Structure
Synonym:

Vistusertib

Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
50mg USD 340  USD340 In stock
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Quality Control
Biological Activity

AZD2014 is a novel dual mTORC1 and mTORC2 inhibitor with potential antineoplastic activity. AZD2014 inhibits biomarkers pAKTSer473 and pNDRG1Thr346. AZD2014 has broad antiproliferative activity across multiple tumour cell lines. AZD2014 induces growth inhibition and cell death in breast cancer cell lines, including ER+ cell lines with acquired resistance to hormone therapy. AZD2014 induces tumour growth inhibition against several xenograft models including a human primary explant model of ER+ breast cancer refractory to tamoxifen.

Customer Product Validations & Biological Datas
Source Cell Physiol Biochem (2018). Figure 4. AZD2014
Method Flow cytometric analysis
Cell Lines NSCLC cell
Concentrations -
Incubation Time 24 h
Results When mTOR was inhibited in anti-miR-99a-A549 cells by AZD2014, the cells became more sensitive to radiation than control cells and the levels of anti-apoptosis markers were reduced
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 462.54
Formula C25H30N6O3
CAS Number 1009298-59-2
Purity >98%
Solubility DMSO 18 mg/mL
Storage at -20°C
References

[1] Byung-Hyun Cha, et al. AZD2014, a dual mTOR inhibitor, attenuates cardiac hypertrophy in vitro and in vivo

[2] Ruyu Pi, et al. Dual mTORC1/2 inhibitor AZD2014 diminishes myeloid-derived suppressor cells accumulation in ovarian cancer and delays tumor growth

[3] H Liao, et al. Antitumor effects of AZD2014, a dual mTORC1/2 inhibitor, against human hepatocellular carcinoma xenograft in nude mice

[4] Julien Bensalem, et al. Inhibiting mTOR activity using AZD2014 increases autophagy in the mouse cerebral cortex

[5] Senmao Li, et al. Potent antitumour of the mTORC1/2 dual inhibitor AZD2014 in docetaxel-sensitive and docetaxel-resistant castration-resistant prostate cancer cells

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Keywords: AZD2014, Vistusertib supplier, mTOR, inhibitors

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