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521235

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

Name: PDGFR Tyrosine Kinase Inhibitor VI, SU6668 - CAS 210644-62-5 - Calbiochem
Brand: MM

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

This product is discontinued. Contact Technical Servicefor assistance.

Quality Level

100

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

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-

InChI key

NHFDRBXTEDBWCZ-ZROIWOOFSA-N

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).

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

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

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

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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Antiangiogenic therapy targeting the tyrosine kinase receptor for vascular endothelial growth factor receptor inhibits the growth of colon cancer liver metastasis and induces tumor and endothelial cell apoptosis.

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.

Proteomic characterization of the angiogenesis inhibitor SU6668 reveals multiple impacts on cellular kinase signaling.

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

The antiangiogenic protein kinase inhibitors SU5416 and SU6668 inhibit the SCF receptor (c-kit) in a human myeloid leukemia cell line and in acute myeloid leukemia blasts.

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

Indolinone tyrosine kinase inhibitors block Kit activation and growth of small cell lung cancer cells.

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

SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice.

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.

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