[CAS NO. 2417089-74-6]  XL177A

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PRODUCTS SPECIFICATIONS [2417089-74-6]

Catalog
HY-138794
Brand
MCE
CAS
2417089-74-6

DESCRIPTION [2417089-74-6]

Overview

MDL-
Molecular Weight861.47
Molecular FormulaC48H57ClN8O5
SMILESO=C(C(C=CC1=C2Cl)=CC1=NC3=C2CCCC3)NCCC[C@@H](CC4=CC=CC=C4)C(N5CCC(CN6C=NC7=C(C=CC(NC(CCN8CCN(C)CC8)=O)=C7)C6=O)(O)CC5)=O

For research use only. We do not sell to patients.

Summary

XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC 50 of 0.34 nM. XL177A elicits cancer cell killing through a p53-dependent mechanism [1] .


In Vitro

XL177A is a potent USP7 inhibitor and p53 stabilizer in cyto. XL177A suppresses cancer cell growth predominantly through a p53-dependent mechanism. XL177A labels the catalytic cysteine, C223, of USP7 with exquisite selectivity for USP7 across the DUBome and human proteome [1] .
XL177A (1 μM) induces complete G1 arrest in MCF7 cells after 24 hours [1] .
Treatment of MCF7 cells, which express WT TP53, with XL177A (0.001- 10 μM) induces rapid degradation of HDM2 within 2 hours, followed by increases in p53 and downstream p21 protein levels [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis [1]

Cell Line: MCF7 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 18-24 hours
Result: The p53 and p21 protein levels remained high, but MDM2 protein levels matched DMSO control.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 29.02 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1608 mL 5.8040 mL 11.6081 mL
5 mM 0.2322 mL 1.1608 mL 2.3216 mL
10 mM 0.1161 mL 0.5804 mL 1.1608 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (2.41 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.41 mM); Clear solution

* All of the co-solvents are available by MCE.