Home PI3K/Akt/mTOR mTOR inhibitor XL388 For research use only.

XL388

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 Chemical Structure

XL388 Chemical Structure

CAS No. 1251156-08-7

Purity & Quality Control

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

XL388 Related Products

Signaling Pathway

mTOR Signaling Pathways

mTOR Signaling Pathway

Biological Activity

Description 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.
Targets
mTORC1 [1] mTOR [2] mTORC2 [1]
8 nM 9.9 nM 166 nM
In vitro
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, XL388 inhibits the viability of solid and hematopoietic tumor cell lines. The proliferation IC50 is 1.37 μM in MCF-7 cell line. XL388 also synergizes with chemotherapeutics in cell-based assays to block cell viability. [1]
In Vivo
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. [1] XL388 displays good pharmacokinetics and oral exposure in multiple species with moderate bioavailability. The mean plasma protein binding of XL388 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 XL388 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.[2]
Animal Research Animal Models MCF-7 xenograft tumors
Dosages 50, 100 mg/kg once daily
Administration Orally

Chemical Information & Solubility

Molecular Weight 455.5 Formula

C23H22FN3O4S
CAS No. 1251156-08-7 SDF Download XL388 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 1.25 mg/mL ( (2.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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