Chemdea |
Ku-0063794 – mTOR Inhibitor |
Catalog # CD0274 |
Price: 1 mg - $29; 5 mg - $43; 10 mg - $78; 25
mg - $171; 50 mg - $243; 100 mg - $464; 200 mg - $844, 1 g - $2979 Shipping and handling fee: Within USA - $15; International - $39; Delivery by FedEx |
Availability: In stock |
rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
Pale yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT
GAS. Purity: 99% by HPLC. CAS#
938440-64-3. Solubility: DMSO
(15 mg/mL). Molecular Formula: C25H31N5O4.
Molecular Weight: 465.5. Ku-0063794 inhibits both mTORC1 and mTORC2 with an
IC50 of ∼10 nM, but does not suppress the activity of 76
other protein kinases or seven lipid kinases, including Class 1 PI3Ks at
1000-fold higher concentrations. Ku-0063794 is cell permeant, suppresses
activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not
RSK (ribosomal S6 kinase). Ku-0063794 also suppressed cell growth and induced
a G1-cell-cycle arrest. Ku-0063794 is a prototype of mTOR inhibitor AZD8055
currently in Phase I/II trial in Advance Solid Tumors, Lymphoma and
Endometrial Carcinoma.
Reference: García‑Martínez, J. M. et al. Biochem J. 2009, 421, 29. |
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