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50440-30-7

50440-30-7 structure
50440-30-7 structure
  • Name: T3Inh-1
  • Chemical Name: 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide
  • CAS Number: 50440-30-7
  • Molecular Formula: C27H20N6O3
  • Molecular Weight: 476.48600
  • Catalog: Research Areas Cancer
  • Create Date: 2017-07-24 22:11:46
  • Modify Date: 2024-01-03 14:08:11
  • T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream)[1].

Name 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide
Synonyms hms2860i06
Description T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream)[1].
Related Catalog
In Vitro T3Inh-1 (5 µM; 24-48 hours; 5 µM; MDA-MB231 cells) is strikingly effective, inhibiting migration by >80% and invasion by 98% while causing no discernable effect on cell proliferation[1]. T3Inh-1 exhibits no toxicity and did not affect HEK cell proliferation[1]. T3Inh-1 (HEK cells; 6 hours)increases cleavage of FGF23[1].
In Vivo T3Inh-1 (25 or 50 mg/kg; i.p.) blocks ppGalNAc-T3-mediated glycan-masking of FGF23 thereby increasing its cleavage[1]. Animal Model: Wild-type C57BL/6 six to eight week old mice[1] Dosage: 25 or 50 mg/kg Administration: Intraperitoneal injection (Dissolved in DMSO at 25 and 50 mg/ml then further diluted with PEG400 to create 5 and 10 mg/ml stocks for injection) Result: Caused a robust and statistically significant increase the ratio of cleaved/intact FGF23 at the tested 25 and 50 mg/kg concentrations.
References

[1]. Song L, et al. Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels. Elife. 2017;6:e24051. Published 2017 Mar 31.

Density 1.431g/cm3
Boiling Point 662.7ºC at 760mmHg
Molecular Formula C27H20N6O3
Molecular Weight 476.48600
Flash Point 354.6ºC
Exact Mass 476.16000
PSA 124.76000
LogP 7.01970
Index of Refraction 1.783
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