XL177A

XL177A is a potent USP7 inhibitor. 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.

Product information

CAS Number: 2417089-74-6

Molecular Weight: 861.47

Formula: C48H57ClN8O5

Chemical Name: (S)-N-(4-benzyl-5-(4-hydroxy-4-((7-(3-(4-methylpiperazin-1-yl)propanamido)-4-oxoquinazolin-3(4H)-yl)methyl)piperidin-1-yl)-5-oxopentyl)-9-chloro-5, 6, 7, 8-tetrahydroacridine-3-carboxamide

Smiles: CN1CCN(CCC(=O)NC2=CC3N=CN(CC4(O)CCN(CC4)C(=O)[C@H](CC4C=CC=CC=4)CCCNC(=O)C4=CC5=NC6CCCCC=6C(Cl)=C5C=C4)C(=O)C=3C=C2)CC1

InChiKey: UYJWYMWIVMCGQZ-DHUJRADRSA-N

InChi: InChI=1S/C48H57ClN8O5/c1-54-24-26-55(27-25-54)21-17-43(58)52-36-14-16-39-41(30-36)51-32-57(47(39)61)31-48(62)18-22-56(23-19-48)46(60)35(28-33-8-3-2-4-9-33)10-7-20-50-45(59)34-13-15-38-42(29-34)53-40-12-6-5-11-37(40)44(38)49/h2-4,8-9,13-16,29-30,32,35,62H,5-7,10-12,17-28,31H2,1H3,(H,50,59)(H,52,58)/t35-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (117.72 mM) Ethanol : 100 mg/mL (117.72 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

References:

1. Nathan J Schauer, et al. Sci Rep. 2020 Mar 24;10(1):5324.

Products are for research use only. Not for human use.