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Merck
CN

572660

SU11652

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

别名:

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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关于此项目

经验公式(希尔记法):
C22H27ClN4O2
化学文摘社编号:
分子量:
414.93
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze
protect from light
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产品名称

SU11652, A cell-permeable pyrrole-indolinone compound that acts as a potent, reversible, and ATP-competitive tyrosine kinase receptor and angiogenic inhibitor.

color

orange

SMILES string

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-

InChI key

XPLJEFSRINKZLC-ATVHPVEESA-N

assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

solubility

DMSO: 4 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

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

Disclaimer

Toxicity: Standard Handling (A)

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.

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.

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 1


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