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XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $97 | In Stock | |
5 mg | $197 | In Stock | |
10 mg | $313 | In Stock | |
25 mg | $533 | In Stock | |
50 mg | $768 | In Stock | |
100 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $297 | In Stock |
Description | XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism. |
Targets&IC50 | USP7:0.34 nM |
In vitro | XL177A irreversibly inhibits USP7 with sub-nM potency and selectivity across the human proteome.?Evaluation of the cellular effects of XL177A reveals that selective USP7 inhibition suppresses cancer cell growth predominantly through a p53-dependent mechanism:?XL177A specifically upregulates p53 transcriptional targets transcriptome-wide, hotspot mutations in TP53 but not any other genes predict response to XL177A across a panel of ~500 cancer cell lines, and TP53 knockout rescues XL177A-mediated growth suppression of TP53 wild-type (WT) cells.?Together, these findings suggest TP53 mutational status as a biomarker for response to USP7 inhibition.?We find that Ewing sarcoma and malignant rhabdoid tumor (MRT), two pediatric cancers that are sensitive to other p53-dependent cytotoxic drugs, also display increased sensitivity to XL177A. |
Molecular Weight | 861.47 |
Formula | C48H57ClN8O5 |
Cas No. | 2417089-74-6 |
Smiles | CN1CCN(CCC(=O)Nc2ccc3c(c2)ncn(CC2(O)CCN(CC2)C(=O)[C@@H](CCCNC(=O)c2ccc4c(Cl)c5CCCCc5nc4c2)Cc2ccccc2)c3=O)CC1 |
Relative Density. | 1.35 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/ml (63.84 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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