Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

Product information

CAS Number: 161552-03-0

Molecular Weight: 603.67

Formula: C27H41N9O7

Chemical Name: 2-[8-(4-aminobutyl)-5-benzyl-11-{3-[(diaminomethylidene)amino]propyl}-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetic acid

Smiles: NC(N)=NCCCC1NC(=O)C(CCCCN)NC(=O)C(CC2C=CC=CC=2)NC(=O)C(CC(O)=O)NC(=O)CNC1=O

InChiKey: NVHPXYIRNJFKTE-UHFFFAOYSA-N

InChi: InChI=1S/C27H41N9O7/c28-11-5-4-9-18-24(41)34-17(10-6-12-31-27(29)30)23(40)32-15-21(37)33-20(14-22(38)39)26(43)36-19(25(42)35-18)13-16-7-2-1-3-8-16/h1-3,7-8,17-20H,4-6,9-15,28H2,(H,32,40)(H,33,37)(H,34,41)(H,35,42)(H,36,43)(H,38,39)(H4,29,30,31)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 250 mg/mL (414.13 mM; Need ultrasonic). H2O : 50 mg/mL (82.83 mM; Need ultrasonic).

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:

Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with a IC50 of 0.94 nM. [66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation.

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