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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

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About This Item

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

Key Documents

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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’.

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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.
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
B D Smolich et al.
Blood, 97(5), 1413-1421 (2001-02-27)
SU5416 and SU6668 are potent antiangiogenic small-molecule inhibitors of receptor tyrosine kinases, including those of the vascular endothelial growth factor and platelet-derived growth factor receptor families. The stem cell factor (SCF) receptor, c-kit, is structurally related to these receptors and
G W Krystal et al.
Cancer research, 61(9), 3660-3668 (2001-04-28)
Six indolinone tyrosine kinase inhibitors were characterized for their ability to inhibit Kit kinase and for their effects on the growth of small cell lung cancer (SCLC) cell lines. All of the six compounds were potent inhibitors of Kit kinase
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
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