In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 64.9, 42.1, 10.6, and 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), and S6RP(pS240/242), respectively.
LY3023414 is an ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
The phosphoinositide-3 kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) pathway is one of the most frequently altered pathways in cancer cell growth and survival.
In vitro: In biochemical testing against approximately 266 kinases, LY3023414 was found to potently and selectively inhibit class I PI3K isoforms, mTORC1/2, as well as DNA-PK at low concentrations. In addition, inhibition of PI3K/AKT/mTOR signaling by LY3023414 led to G1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel .
In vivo: LY3023414 showed high bioavailability and dose-dependent dephosphorylation of PI3K/AKT/mTOR pathway downstream substrates for 4 to 6 hours, indicating LY3023414's half-life of 2 hours. Moreover, equivalent total daily doses of LY3023414 given either once or twice daily could inhibit tumor growth to the similar extents in multiple xenograft models, demonstrating intermittent target inhibition was sufficient for antitumor activity .
Clinical trial: LY3023414 appears to be safe when administered as single agent up to 325 mg QD or 200 mg BID. Currently, LY3023414 is investigated in tumor-specific expansion cohorts for breast cancer, mesothelioma, Non-Hodgkin Lymphoma as well as NSCLC (Clinical trial information: NCT01655225).
 Smith MC,Mader MM,Cook JA,et al. Characterization of LY3023414, a Novel PI3K/mTOR Dual Inhibitor Eliciting Transient Target Modulation to Impede Tumor Growth. Mol Cancer Ther.2016 Oct;15(10):2344-2356.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥40.6mg/mL in DMSO|
|Canonical SMILES||O=C(N(C1=C2C3=CC(C4=CC(C(O)(C)C)=CN=C4)=CC=C3N=C1)C)N2C[[email protected]](C)OC|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
Quality Control & MSDS
- View current batch:
Purity = 99.55%
- COA (Certificate Of Analysis)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)