Cyclo(RGDyK)αVβ3 integrin inhibitor CAS# 250612-42-1 |
- MNS
Catalog No.:BCC3943
CAS No.:1485-00-3
- BIO 1211
Catalog No.:BCC3945
CAS No.:187735-94-0
- Cilengitide
Catalog No.:BCC3942
CAS No.:188968-51-6
- A 205804
Catalog No.:BCC3944
CAS No.:251992-66-2
- Firategrast
Catalog No.:BCC1575
CAS No.:402567-16-2
- Zaurategrast
Catalog No.:BCC2070
CAS No.:455264-31-0
Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products

Cas No. | 250612-42-1 | SDF | Download SDF |
PubChem ID | 129626569 | Appearance | Powder |
Formula | C31H43F6N9O12 | M.Wt | 847.72 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : ≥ 130 mg/mL (153.35 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 2-[(2R,5S,8R,11R)-8-(4-aminobutyl)-11-[3-(diaminomethylideneamino)propyl]-5-[(4-hydroxyphenyl)methyl]-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid;2,2,2-trifluoroacetic acid | ||
SMILES | C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCN=C(N)N)CCCCN)CC2=CC=C(C=C2)O)CC(=O)O.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O | ||
Standard InChIKey | CDDUWKKOPQABPG-WVSPKWNLSA-N | ||
Standard InChI | InChI=1S/C27H41N9O8.2C2HF3O2/c28-10-2-1-4-18-24(42)34-17(5-3-11-31-27(29)30)23(41)32-14-21(38)33-20(13-22(39)40)26(44)36-19(25(43)35-18)12-15-6-8-16(37)9-7-15;2*3-2(4,5)1(6)7/h6-9,17-20,37H,1-5,10-14,28H2,(H,32,41)(H,33,38)(H,34,42)(H,35,43)(H,36,44)(H,39,40)(H4,29,30,31);2*(H,6,7)/t17-,18-,19+,20-;;/m1../s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |

Cyclo(RGDyK) Dilution Calculator

Cyclo(RGDyK) Molarity Calculator

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland

TsingHua University

The University of Michigan

Miami University

DRURY University

Jilin University

Fudan University

Wuhan University

Sun Yat-sen University

Universite de Paris

Deemed University

Auckland University

The University of Tokyo

Korea University
Target: αVβ3 integrin
IC50: 20 nM
Cyclo(RGDyK) is a selective and potent αVβ3 integrin inhibitor with IC50 value of 20 nM [1]. The αVβ3 integrin, expressed on various malignant human tumors and on endothelial cells, plays an important role in tumor-induced angiogenesis and tumor metastasis. Therefore, αVβ3 integrin is a potential therapeutic target for tumor disease. Inhibition of αVβ3 integrin by αVβ3 antagonists not only blocked blood vessel formation but further led to tumor regression [1].
In vitro: Cyclo(RGDyK) conjugation facilitated intracellular drug delivery of polymeric micelles to neovasculature (HUVECs) and tumor cells in which integrin is overexpressed [2]. In addition, Cyclo(RGDyK) showed high affinity and selectivity for αVβ3 integrin over αVβ5 and αIIbβ3 [1].
In vivo: Cyclo(RGDyK) (1 nM, i.v. injection) blocked the increase of αVβ3 integrin expression in the intima of the left stenotic carotid artery of apoE-/- mice [2].
References:
1. Haubner R, Wester HJ, Burkhart F, Senekowitsch-Schmidtke R, Weber W, Goodman SL, et al. Glycosylated RGD-containing peptides: tracer for tumor targeting and angiogenesis imaging with improved biokinetics. J Nucl Med. 2001;42(2):326-36.
2. Yin J, Li Z, Yang T, Wang J, Zhang X, Zhang Q. Cyclic RGDyK conjugation facilitates intracellular drug delivery of polymeric micelles to integrin-overexpressing tumor cells and neovasculature. J Drug Target. 2011;19(1):25-36.
- (±)-Acetylcarnitine chloride
Catalog No.:BCC6617
CAS No.:2504-11-2
- Excavatin M
Catalog No.:BCN5116
CAS No.:250293-31-3
- PNU 177864 hydrochloride
Catalog No.:BCC7664
CAS No.:250266-51-4
- Boc-His(Dnp)-OH
Catalog No.:BCC3401
CAS No.:25024-53-7
- Otophylloside F
Catalog No.:BCN6441
CAS No.:250217-73-3
- 1,2:4,5-Di-O-isopropylidene-beta-D-fructopyranose
Catalog No.:BCN1475
CAS No.:25018-67-1
- Miriplatin hydrate
Catalog No.:BCC1751
CAS No.:250159-48-9
- Anamorelin
Catalog No.:BCC1362
CAS No.:249921-19-5
- Borreriagenin
Catalog No.:BCN5115
CAS No.:249916-07-2
-
SB-334867 hydrochloride
Catalog No.:BCC4289
CAS No.:249889-64-3
- 1,2-Benzanthraquinone
Catalog No.:BCC8410
CAS No.:2498-66-0
- 2beta-Hydroxygrandiflorenic acid
Catalog No.:BCN8447
CAS No.:24967-93-9
- Pedunsaponin A
Catalog No.:BCN8192
CAS No.:250613-27-5
- NNC 63-0532
Catalog No.:BCC7177
CAS No.:250685-44-0
- Salvisyrianone
Catalog No.:BCN4821
CAS No.:250691-57-7
- Antazoline HCl
Catalog No.:BCC4627
CAS No.:2508-72-7
- FRATide
Catalog No.:BCC5821
CAS No.:251087-38-4
- Crebanine
Catalog No.:BCN5117
CAS No.:25127-29-1
- Urotensin II (human)
Catalog No.:BCC5796
CAS No.:251293-28-4
- SU 16f
Catalog No.:BCC7639
CAS No.:251356-45-3
- M344
Catalog No.:BCC2162
CAS No.:251456-60-7
- Tesaglitazar
Catalog No.:BCC7828
CAS No.:251565-85-2
- 5-Chloro-2-nitrobenzoic acid
Catalog No.:BCC8743
CAS No.:2516-95-2
- Acevaltrate
Catalog No.:BCN7127
CAS No.:25161-41-5