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XL177A

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Catalog No. T9122Cas No. 2417089-74-6

XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.

XL177A

XL177A

🥰Excellent
Purity: 98.75%
Catalog No. T9122Cas No. 2417089-74-6
XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.
Pack SizePriceAvailabilityQuantity
1 mg$97In Stock
5 mg$197In Stock
10 mg$313In Stock
25 mg$533In Stock
50 mg$768In Stock
100 mg$1,080In Stock
1 mL x 10 mM (in DMSO)$297In Stock
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Purity:98.75%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight861.47
FormulaC48H57ClN8O5
Cas No.2417089-74-6
SmilesCN1CCN(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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.1608 mL5.8040 mL11.6081 mL58.0403 mL
5 mM0.2322 mL1.1608 mL2.3216 mL11.6081 mL
10 mM0.1161 mL0.5804 mL1.1608 mL5.8040 mL
20 mM0.0580 mL0.2902 mL0.5804 mL2.9020 mL
50 mM0.0232 mL0.1161 mL0.2322 mL1.1608 mL

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