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145697 WYE 687 Dihydrochloride (Potent and Selective mTOR Inhibitor, N-[4-[4-(4-Morpholinyl)-1-[1-(3-pyr idinylmethyl)-4-piperidinyl]-1H-pyrazolo[3,4-d]pyr imidin-6-yl]phenyl]-carbamic acid methyl ester hydrochloride) CAS: 1062161-90-3

Specifications
References
CAS Number
1062161-90-3
Grade
Highly Purified
Molecular Formula
C28H32N8O3
Molecular Weight
601.53
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
RT

Potent, ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) (IC50 = 7nm). Displays selectivity for mTOR over PI 3-Kalpha (~100-fold) and PI 3-Kgamma (~500-fold). Inhibits phosphorylation of mTORC1 and mTORC2 substrates including S6K, SGK and Akt; blocks VEGF secretion and HIF-1alpha expression. Exhibits antiproliferative effects in cancer cell lines through G1 cell cycle arrest and selective apoptosis.

Sequence
C28H32N8O3
Solubility
DMSO (~100mM), H2O (~100mM)
Molecular Weight
~601.53
Storage and Stability
May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Purity
~98% (HPLC)
Concentration
Not determined
Form
Supplied as a pale brown solid.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
References
1. Yu et al (2009) Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer.Res. 69 (15) 6232. PMID: 19584280.
USBio References
No references available
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