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XL388

Cat. No. M2118
XL388 Structure
Size Price Availability Quantity
5mg USD 240 In stock
10mg USD 320 In stock
50mg USD 990 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

XL388 is a novel class of highly potent and selective, ATP-competitive inhibitor of the mammalian target of rapamycin (mTOR). XL388 inhibited cellular phosphorylation of mTOR complex 1 (p-p70S6K, pS6, and p-4E-BP1) and mTOR complex 2 (pAKT (S473)) substrates. Furthermore, XL388 displayed good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. Oral administration of XL388 to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 455.5
Formula C23H22FN3O4S
CAS Number 1251156-08-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Takeuchi CS, et al. J Med Chem. 2013 Mar 28;56(6):2218-34. PMID: 23394126.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: XL388 supplier, mTOR, inhibitors

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