572660

SU11652

A cell-permeable pyrrole-indolinone compound that acts as a potent, reversible, and ATP-competitive tyrosine kinase receptor and angiogenic inhibitor.

• Sinonimo/i: SU11652, 5-[(Z)-(5-Chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, PDGFR Tyrosine Kinase Inhibitor VIII, VEGFR Tyrosine Kinase Inhibitor XVII, VEGFR2 Kinase Inhibitor XIV
• Formula empirica (notazione di Hill): C₂₂H₂₇ClN₄O₂
• Numero CAS: 326914-10-7
• Peso molecolare: 414.93
• Numero MDL: MFCD09037560
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Stato: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: orange
• Solubilità: DMSO: 4 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: Clc1cc2c(cc1)NC(=O)\C\2=C/c3[nH]c(c(c3C)C(=O)NCCN(CC)CC)C
• InChI: 1S/C22H27ClN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-; XPLJEFSRINKZLC-ATVHPVEESA-N

Descrizione

Descrizione generale

A cell-permeable pyrrole-indolinone compound that acts as a potent, reversible, and ATP-competitive tyrosine kinase receptor and angiogenic inhibitor that exhibits greater selectivity for PDGFRβ (IC₅₀ = 3 nM), VEGFR2 (IC₅₀ = 27 nM), FGFR1 (IC₅₀ = 170 nM), and Kit family members (IC₅₀ = ~ 10-500 nM) over EGFR (IC₅₀ >20 µM). Reported to display anti-proliferative and pro-apoptotic properties in tumor cells.

A cell-permeable, potent, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of PDGFRβ (IC₅₀ = 3 nM), VEGFR2 (IC₅₀ = 27 nM), FGFR1 (IC₅₀ = 170 nM), and Kit family members (IC₅₀ ~10-500 nM). Does not effect the activity of EGFR (IC₅₀ >20 µM). Reported to display anti-proliferative, antiangiogenic and pro-apoptotic properties in tumor cells.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
PDGFRB

Product competes with ATP.

Reversible: yes

Target IC₅₀: 3 nM, 27 nM, 170 nM against PDGFRβ, VEGFR2, and FGFR1, respectively

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Altre note

Heryanto, B., et al. 2003. Reproduction125, 334.
Sun, L., et al. 2003. J. Med. Chem.46, 1116.
Liao, A.T., et al. 2002. Blood100, 585.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1