Skip to Content
Merck

521235

PDGFR Tyrosine Kinase Inhibitor VI, SU6668 - CAS 210644-62-5 - Calbiochem

The PDGFR Tyrosine Kinase Inhibitor VI, SU6668, also referenced under CAS 210644-62-5, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

PDGFR Tyrosine Kinase Inhibitor VI, SU6668 - CAS 210644-62-5 - Calbiochem, (Z)-3-(2,4-Dimethyl-5-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl)-propionic acid, mTOR Inhibitor X, VEGFR Tyrosine Kinase Inhibitor XXVII, VEGFR2 Kinase Inhibitor XXV, Aurora Kinase Inhibitor IV

Sign In to View Organizational & Contract Pricing.

Select a Size

About This Item

Empirical Formula (Hill Notation):
C18H18N2O3
CAS Number:
210644-62-5
Molecular Weight:
310.35
UNSPSC Code:
12352200

Key Documents

View All Documentation
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

Product Name

PDGFR Tyrosine Kinase Inhibitor VI, SU6668 - CAS 210644-62-5 - Calbiochem, The PDGFR Tyrosine Kinase Inhibitor VI, SU6668, also referenced under CAS 210644-62-5, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

InChI key

NHFDRBXTEDBWCZ-ZROIWOOFSA-N

InChI

1S/C18H18N2O3/c1-10-12(7-8-17(21)22)11(2)19-16(10)9-14-13-5-3-4-6-15(13)20-18(14)23/h3-6,9,19H,7-8H2,1-2H3,(H,20,23)(H,21,22)/b14-9-

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

dark yellow

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Disclaimer

Toxicity: Harmful (C)

General description

A cell-permeable indolinone compound that acts as a potent ATP-competitive inhibitor against RTKs (receptor tyrosine kinases) Kit, PDGFRβ, VEGFR2 (Flk-1/KDR), FGFR1 activity in vitro (IC50 = 0.01, 0.1, 3.9, and 3.8 µM, respectively) and PDGF/VEGF/bFGF-mediated angiogenesis and tumor development in vivo. Although initially characterized as an RTK inhibitor, SU6668 is now also known to target ser/thr kinases Aurora A, Aurora B, TBK1 (NAK/T2K), and AMPK (IC50 = 0.85, 0.047, 1.4, and 1.8 µM, respectively), as well as non-receptor TKs Lyn and Yes (IC50 = 4.3 and 5.8 µM, respectively).

Other Notes

Godl, K., et al. 2005. Cancer Res.65, 6919.
Laird, A.D., et al. 2002. FASEB J.16, 681.
Krystal, G.W., et al. 2001. Cancer Res.61, 3660.
Smolich, B.D., et al. 2001. Blood97, 1413.
Laird, A.D., et al. 2000. Cancer Res.60, 4152.
Shaheen, R.M., et al. 1999. Cancer Res.59, 5412.
Sun, L. et al. 1999. J. Med. Chem.42, 5120.

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

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

A Douglas Laird et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 16(7), 681-690 (2002-04-30)
SU6668 is a small molecule inhibitor of the angiogenic receptor tyrosine kinases Flk-1/KDR, PDGFRbeta, and FGFR1. In mice, SU6668 treatment resulted in regression or growth arrest of all large established human tumor xenografts examined associated with loss of tumor cellularity.
A D Laird et al.
Cancer research, 60(15), 4152-4160 (2000-08-17)
Vascular endothelial growth factor, fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. Using rational drug design coupled with traditional screening technologies, we have discovered
R M Shaheen et al.
Cancer research, 59(21), 5412-5416 (1999-12-20)
Increased vascular endothelial growth factor (VEGF) expression is associated with colon cancer metastases. We hypothesized that inhibition of VEGF receptor activity could inhibit colon cancer liver metastases. BALB/c mice underwent splenic injection with CT-26 colon cancer cells to generate metastases.
Klaus Godl et al.
Cancer research, 65(15), 6919-6926 (2005-08-03)
Knowledge about molecular drug action is critical for the development of protein kinase inhibitors for cancer therapy. Here, we establish a chemical proteomic approach to profile the anticancer drug SU6668, which was originally designed as a selective inhibitor of receptor
L Sun et al.
Journal of medicinal chemistry, 42(25), 5120-5130 (1999-12-22)
Receptor tyrosine kinases (RTKs) have been implicated as therapeutic targets for the treatment of human diseases including cancers, inflammatory diseases, cardiovascular diseases including arterial restenosis, and fibrotic diseases of the lung, liver, and kidney. Three classes of 3-substituted indolin-2-ones containing
View All Related Papers

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service