Brief Description

XL388 is a novel, highly potent, selective, and ATP-competitive mammalian target of rapamycin (mTOR) inhibitor with IC50 of 9.9 nM; 1000-fold selectivity over the closely related PI3K kinases.
IC50 Value: 9.9 nM [1]
Target: mTOR
in vitro: Compound 28 (XL388) inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates.Furthermore, this compound 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 [1].
in vivo: XL388 resulted in complete inhibition of MCF-7 xenograft tumor growth at both doses, with significant tumor regression of 22% and 40% below pretreatment values at the 50 and 100 mg/kg doses, respectively. Furthermore, 28 does not appear to show significant toxicity. Mice in the 50 mg/kg cohort over the course of the study gained on average 2.2% additional mass, while those in the 100 mg/kg cohort lost on average 2.8% of their body mass [1].
References on XL388:
[1]. Craig S. Takeuchi, Byung Gyu Kim, Discovery of a Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR). J. Med. Chem., 2013, 56 (6), pp 2218-2234

Solubility

in DMSO > 10 mM

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid