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Chemdea |
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WYE-132 / WYE-125132 – sub-nanomolar
mTOR Inhibitor |
Catalog # CD0325 |
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Price: 1 mg - $95;
5 mg - $195; 10 mg - $270; 25 mg - $525; 50 mg - $750; 100 mg - $1250 |
Availability: Inquire |
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1-{4-[1-(1,4-Dioxa-spiro[4.5]dec-8-yl)-4-(8-oxa-3-aza-bicyclo[3.2.1]oct-3-yl)-1H-pyrazolo[3,4-d] pyrimidin-6-yl]-phenyl}-3-methyl-urea
White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity > 99% by HPLC. CAS# 1144068-46-1. Solubility: DMSO (50 mg/mL). Molecular Formula: C27H33N7O4. Molecular Weight: 519.60.
WYE-132 (WYE-125132) is a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks). WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. WYE-132 targeted P-AKT(S473) and AKT function without significantly reducing the steady-state level of the PI3K/PDK1 activity biomarker P-AKT(T308), highlighting a prominent and direct regulation of AKT by mTORC2 in cancer cells. Compared with the rapalog temsirolimus/CCI-779, WYE-132 elicited a substantially stronger inhibition of cancer cell growth and survival, protein synthesis, cell size, bioenergetic metabolism, and adaptation to hypoxia. Oral administration of WYE-132 to tumor-bearing mice showed potent single-agent antitumor activity against MDA361 breast, U87MG glioma, A549 and H1975 lung, as well as A498 and 786-O renal tumors. An optimal dose of WYE-132 achieved a substantial regression of MDA361 and A549 large tumors and caused complete regression of A498 large tumors when co-administered with bevacizumab. References: 1. Yu, K., et al. Cancer Res 2010, 70, 621; 2. Curran, J. K., et al. Bioorg. Med. Chem. Lett. 2010, 20, 1440; 3. Shor, B. et al. J. Biol. Chem. 2010, 285, 15380. |
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CHEMDEA; |