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XL388

Cat. No. M2118
XL388 Structure
Size Price Availability Quantity
5mg USD 110  USD110 In stock
10mg USD 170  USD170 In stock
25mg USD 350  USD350 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 455.5
Formula C23H22FN3O4S
CAS Number 1251156-08-7
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Takeuchi CS, et al. J Med Chem. Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).

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Keywords: XL388 supplier, mTOR, inhibitors, activators


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