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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $97 | In Stock | In Stock | |
| 5 mg | $197 | In Stock | In Stock | |
| 10 mg | $313 | In Stock | In Stock | |
| 25 mg | $533 | In Stock | In Stock | |
| 50 mg | $768 | - | In Stock | |
| 100 mg | $1,080 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $297 | In Stock | 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 | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (63.84 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.32 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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