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Datasheet of XL388
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. 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. 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.
Chemical Information Catalog
DC3123
Purity of current batch:
>98%
Molecular Weight (MW)
455.5
Molecular Formula
C23H22FN3O4S
CAS No.
1251156-08-7
Solubility (25째C)
DMSO
Storage
Store at -20째C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20째C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.