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Sigma-Aldrich

SU11652

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C22H27ClN4O2
CAS Number:
326914-10-7
Molecular Weight:
414.93
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange

solubility

DMSO: 4 mg/mL

shipped in

ambient

storage temp.

2-8°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-

InChI key

XPLJEFSRINKZLC-ATVHPVEESA-N

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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.

Legal Information

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

WGK

WGK 1

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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