XL 388

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Cat.No. 4893 - XL 388 | C23H22FN3O4S | CAS No. 1251156-08-7
Description: Potent and selective mTOR inhibitor; antitumor
Chemical Name: [7-(6-Amino-3-pyridinyl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]-methanone
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Potent and selective mTOR inhibitor (IC50 = 9.9 nM). Inhibits mTOR activity in an ATP-competitive manner. Exhibits >300-fold selectivity for mTOR over PI 3-K and a range of other kinases. Displays antitumor activity in athymic nude mice implanted with tumor xenografts.

Technical Data

M. Wt 455.5
Formula C23H22FN3O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1251156-08-7
PubChem ID 59604787
InChI Key LNFBAYSBVQBKFR-UHFFFAOYSA-N
Smiles NC1=NC=C(C2=CC=C(OCCN(C(C4=CC=C(S(C)(=O)=O)C(F)=C4C)=O)C3)C3=C2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.6 50

Preparing Stock Solutions

The following data is based on the product molecular weight 455.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.2 mL 10.98 mL 21.95 mL
5 mM 0.44 mL 2.2 mL 4.39 mL
10 mM 0.22 mL 1.1 mL 2.2 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Citations for XL 388

Citations are publications that use Tocris products.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

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  • Nociception
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Pathways for XL 388

mTOR

mTOR Signaling Pathway

mTOR is a serine/threonine kinase that nucleates at multiprotein complexes mTORC1 and mTORC2. Signaling by these complexes regulates cell growth, proliferation and survival.

Protocols

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