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XL-388

Basic information Safety Supplier Related

XL-388 Basic information

Product Name:
XL-388
Synonyms:
  • Methanone, [7-(6-amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-
  • [7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone XL388
  • XL388, >=98%
  • (7-(6-Aminopyridin-3-yl)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)(3-fluoro-2-methyl-4-(methy
  • XL 388
  • XL388
  • XL-388
  • [7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone
CAS:
1251156-08-7
MF:
C23H22FN3O4S
MW:
455.5
Product Categories:
  • PI3K/Akt/mTOR
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
Mol File:
1251156-08-7.mol
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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
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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.

in vivo

To assess the pharmacodynamic effects of XL388 (Compound 28) on the mTOR pathway signaling, athymic nude mice bearing PC-3 prostate tumors are dosed orally at 100 mg/kg of XL388. Rapamycin is also administered intraperitoneally at 5 mg/kg as a reference. Plasma and tumor samples are collected at 1, 4, 8, 16, 24, and 32 h for XL388 and at 4 h for Rapamycin after dosing and homogenized with buffer. Tumor lysates from each animal (n=5) are then pooled for each group and analyzed by immunoblot for levels of phosphorylated p70S6K, S6, 4E-BP1, and AKT. XL388 has moderate terminal elimination half-life (t1/2=1.35 h, 0.45 h, 6.11 h and 0.86 h for mouse (10 mg/kg, iv), rat (3 mg/kg, iv), dog (3 mg/kg, iv), monkey (3 mg/kg, iv))[1].

IC 50

mTOR: 9.9 nM (IC50); mTORC1; mTORC2; DNA-PK: 8.831 μM (IC50)

XL-388Supplier

J & K SCIENTIFIC LTD.
Tel
18210857532
Email
jkinfo@jkchemical.com
Jinan Trio PharmaTech Co., Ltd.
Tel
+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
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XL-388(1251156-08-7)Related Product Information