XL-388 Chemical Properties

Melting point:

>188oC (dec.)

Boiling point:

738.6±60.0 °C(Predicted)

Density 

1.354±0.06 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO (Slightly), Methanol (Slightly)

pka

6.22±0.13(Predicted)

form 

Solid

color 

Off-White to Pale Yellow

Stability:

Hygroscopic

XL-388 Usage And Synthesis

Uses

XL388 is a highly potent, orally bioavailable, selective, ATP-competitive mammalian target of rapamycin (mTOR) inhibitor. XL388 has shown significant and dose-dependent antitumor activity in athymic nude mice implanted with human tumor xenografts.

Biological Activity

XL388 is a potent, selective, orally bioavailable ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) with an IC50 of 9.9 nM for mTOR, 8 nM for mTORC1, 166 nM for mTORC2, and 1000-fold selectivity for mTOR over the closely related PI3K kinases and a panel of 141 protein kinases tested. XL388 blocked mTORC1 phosphorylation of p70S6K (T389) with an IC50 value of 94 nM and blocked mTORC2 phosphorylationof AKT (S473) with an IC50 value of 350 nM. XL388 showed complete tumor growth inhibition in mice bearing MCF-7 xenograft tumors.

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