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XL177A USP7 Inhibitor

Cat.No.S8967

XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
XL177A DUB inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 849.46

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Quality Control

Batch: S896701 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 98.77%
98.77

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (117.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 849.46 Formula

C47H57ClN8O5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2417089-74-6 -- Storage of Stock Solutions

Synonyms N/A Smiles CN1CCN(CC1)CCC(=O)NC2=CC3=C(C=C2)C(=O)N(CC4(O)CCN(CC4)C(=O)C(CCCNC(=O)C5=CC6=C(C=C5)[Cl]=C7CCCCC7=N6)CC8=CC=CC=C8)C=N3

Mechanism of Action

Targets/IC50/Ki
USP7
(Cell-free assay)
0.34 nM
In vitro

Evaluation of the cellular effects of XL177A reveals that selective USP7 inhibition suppresses cancer cell growth predominantly through a p53-dependent mechanism: this compound specifically upregulates p53 transcriptional targets transcriptome-wide, hotspot mutations in TP53 but not any other genes predict response to this inhibitor across a panel of ~500 cancer cell lines, and TP53 knockout rescues its-mediated growth suppression of TP53 wild-type (WT) cells.

References

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