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XL388

Chemical Structure : XL388

CAS No.: 1251156-08-7

XL388 (XL-388)

Catalog No.: PC-49619Not For Human Use, Lab Use Only.

XL388 (XL-388) is a potent, selective and orally bioavailable mTOR inhibitor with IC50 of 9.9 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

XL388 (XL-388) is a potent, selective and orally bioavailable mTOR inhibitor with IC50 of 9.9 nM.
XL388 displays no significant activity against PI3K members with IC50 of >3 uM.
XL388 inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates.
XL388 displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability.
Oral administration of compound 28 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity.

Physicochemical Properties

M.Wt 455.50
Formula C23H22FN3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]methanone

References

1. Takeuchi CS, et al. J Med Chem. 2013 Mar 28;56(6):2218-34.

2. Zhu YR, et al. Oncotarget. 2016 Aug 2;7(31):49527-49538.

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