cyclo-CRVLIR

Chemical Structure : cyclo-CRVLIR

Catalog No.: PC-20008Not For Human Use, Lab Use Only.

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

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Biological Activity

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.
cyclo-CRVLIR is specific for the RBD of p110α and not the other PI3K isoforms, and shows no affinity to KRAS or the structurally-related RAF-RBD.
cyclo-CRVLIR blocks p110α/KRAS interaction using MST assays with Kd of 4.4 uM.
Cyclo-CRVLIR (2, 10 and 50 µM) inhibits AKT phosphorylation (pAKT-Ser473) in human lung cancer cell line H1792.

Physicochemical Properties

M.Wt	728.96
Formula	C31H60N12O6S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1,1'-(((3S,6R,9R,12R,15R,18S)-15-((R)-sec-butyl)-12-isobutyl-9-isopropyl-3-(mercaptomethyl)-4,7,10,13,16-pentaoxo-1-oxa-2,5,8,11,14,17-hexaazacyclooctadecane-6,18-diyl)bis(propane-3,1-diyl))diguanidine

References

1. Ismail M, et al. Sci Rep. 2023 Feb 2;13(1):1889.

cyclo-CRVLIR

Biological Activity

Physicochemical Properties

References

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