Home PI3K/Akt/mTOR mTOR inhibitor XL388

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XL388 mTOR inhibitor

Cat.No.S7035

XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.
XL388 mTOR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 455.5

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Quality Control

Batch: S703501 DMSO]1.25 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.66%
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99.66

Solubility

In vitro
Batch:

DMSO : 1.25 mg/mL (2.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 455.5 Formula

C23H22FN3O4S

 Storage (From the date of receipt)
CAS No. 1251156-08-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=CC(=C1F)S(=O)(=O)C)C(=O)N2CCOC3=C(C2)C=C(C=C3)C4=CN=C(C=C4)N

Mechanism of Action

Targets/IC50/Ki
mTORC1
8 nM
mTOR
9.9 nM
mTORC2
166 nM
In vitro
In MCF-7 cells, XL388 blocks mTORC1 phosphorylation of p70S6K (T389)with an IC50 value of 94 nM and blocks mTORC2 phosphorylationof AKT (S473) with an IC50 value of 350 nM. In vitro, this compound inhibits the viability of solid and hematopoietic tumor cell lines. The proliferation IC50 is 1.37 μM in MCF-7 cell line. It also synergizes with chemotherapeutics in cell-based assays to block cell viability.
In vivo
When dosed orally once daily in mice, XL388 shows robust anti-tumor activity in multiple xenograft models including > 100% tumor growth inhibition in the MCF-7 xenograft model. This compound displays good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. The mean plasma protein binding of this chemical in human, monkey, dog, rat, and mouse plasma is evaluated at 5 μM and is determined to be 86%, 90%, 89%, 85%, and 84%, respectively. Oral administration of this agent to athymic nude mice implanted with human tumor xenografts afforded significant and dose-dependent antitumor activity. Strong inhibition of both mTORC1 and mTORC2 is achieved 4−8 h following administration orally at 100 mg/kg. Modest inhibition (39−45%) of phosphorylation of the PI3K target AKT (T308) is also observed 4−8 h post dose.
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