3-Acridinecarboxamide, 9-chloro-5,6,7,8-tetrahydro-N-[(4S)-5-[4-hydroxy-4-[[7-[[3-(4-methyl-1-piperazinyl)-1-oxopropyl]amino]-4-oxo-3(4H)-quinazolinyl]methyl]-1-piperidinyl]-5-oxo-4-(phenylmethyl)pentyl]- Chemical Properties

Density 

1.35±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 50 mg/mL (58.04 mM; Need ultrasonic)

pka

13.61±0.20(Predicted)

form 

Solid

color 

Off-white to light yellow

3-Acridinecarboxamide, 9-chloro-5,6,7,8-tetrahydro-N-[(4S)-5-[4-hydroxy-4-[[7-[[3-(4-methyl-1-piperazinyl)-1-oxopropyl]amino]-4-oxo-3(4H)-quinazolinyl]methyl]-1-piperidinyl]-5-oxo-4-(phenylmethyl)pentyl]- Usage And Synthesis

Biological Activity

XL177A is a highly potent and selective irreversible USP7 inhibitor with an IC50 of 0.34 nM. XL177A elicits cancer cell killing through a p53-dependent mechanism[1]. 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].

References

[1]. Nathan J Schauer, et al. Selective USP7 inhibition elicits cancer cell killing through a p53-dependent mechanism. Sci Rep.2020 Mar 24;10(1):5324.

3-Acridinecarboxamide, 9-chloro-5,6,7,8-tetrahydro-N-[(4S)-5-[4-hydroxy-4-[[7-[[3-(4-methyl-1-piperazinyl)-1-oxopropyl]amino]-4-oxo-3(4H)-quinazolinyl]methyl]-1-piperidinyl]-5-oxo-4-(phenylmethyl)pentyl]-(2417089-74-6)Related Product Information

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• 2-methoxyethyl 4-((4-(4-chlorophenoxy)-3,5-difluorophenyl)sulfonyl)-3-(hydroxycarbamoyl)piperazine-1-carboxylate