2451298-06-7

2451298-06-7 structure
2451298-06-7 structure
  • Name: P-gp inhibitor 5
  • Chemical Name: P-gp inhibitor 5
  • CAS Number: 2451298-06-7
  • Molecular Formula: C28H20ClNO5S
  • Molecular Weight: 517.98
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel P-glycoprotein
  • Create Date: 2022-08-08 10:52:11
  • Modify Date: 2024-01-12 14:45:54
  • P-gp inhibitor 5 (compound 10) is a potent P-glycoprotein (P-gp) inhibitor with P-gp inhibition fold of 2.5 and 3.0 at 1.25 μM and 2.5 μM. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine and Paclitaxel[1].

Name P-gp inhibitor 5
Description P-gp inhibitor 5 (compound 10) is a potent P-glycoprotein (P-gp) inhibitor with P-gp inhibition fold of 2.5 and 3.0 at 1.25 μM and 2.5 μM. P-gp inhibitor 5 has antiproliferative activity against certain cancer cell lines. P-gp inhibitor 5 is effective in reversing the multidrug resistance (MDR) phenotype in ABCB1/Flp-InTM-293 and KBvin cells by restoring their sensitivity to Vincristine and Paclitaxel[1].
Related Catalog
Target

P-gp[1]

In Vitro P-gp inhibitor 5 (compound 10) has cytotoxic against ABCB1/Flp-InTM-293 and KBvin cells with IC50s of 29.7 and 12.6 μM, respectively[1]. P-gp inhibitor 5 (2.5 and 5 μM) lows the IC50s of KBvin cells for Vincristine to 7.59~36.82 nM, for Paclitaxel to 21.0~79.5 nM, for Doxorubicin to 85.7~111 nM; lows the IC50s of HeLaS3 cells for Vincristine to 2.24~3.91 nM, for Paclitaxel to 8.81~9.58 nM, for Doxorubicin to 102~1260 nM[1].
References

[1]. Hung CC, et al. Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors. Eur J Med Chem. 2020 Sep 1;201:112422.

Molecular Formula C28H20ClNO5S
Molecular Weight 517.98
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