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Src Inhibitor No.5, 5 mg  

Src Inhibitor No.5, 5 mg

4-(3'-Methoxy-6'-chloro-anilino)-6-Methoxy-7-(Morpholino-3-propoxy)-quinazoline

potent inhibitor of c-Src

More details

PKI-SRC-005

Availability: within 3 days

265,00 €

Background: Src Inhibitor No.5 is one of several Src-inhibitor leads and belongs into the quinazoline class of selective inhibitors of c-Src with IC50 of 10 nM in vitro and 310 nM in Src 3T3 assay. It is a close relative of the better known c-Src inhibitor AZM 475271 and shares its in vitro potency against c-Src. It is more than 100 fold selective versus kinase-insert-domain-containing receptor tyrosine kinases (VEGF-R IC50=1,18 µM). Published structure activity relationship studies (SAR) on SKI 606, a Quinolinecarbonitrile-homologue of Src Inhibitor No.5 suggests that it may also inhibit the Abl-kinase with IC50 very similar to c-Src. Also, potent inhibition of related kinases Lck and Yes should be expected.

Chemical formula: C23H27ClN4O4 x 2H20
Molecular Weight: 497,05 g/mol
Purity: > 99%
Appearance: white solid
Solubility:  soluble in DMSO (0,1 M), freely soluble in acetic acid

Also available predissolved at 10 mM in our Src Family Inhibitor Set.

Product specific literature references:

Ple PA, Green TP, Hennequin LF, Curwen J, Fennell M, Allen J, Lambert-Van Der Brempt C, Costello G. (2004) "Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src." J Med Chem. 12;47(4):871-87.

Boschelli DH, Wang YD, Johnson S, Wu B, Ye F, Barrios Sosa AC, Golas JM, Boschelli F. (2004) "7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases." J Med Chem. 47(7):1599-601.

Thaimattam R, Daga PR, Banerjee R, Iqbal J. (2005) "3D-QSAR studies on c-Src kinase inhibitors and docking analyses of a potent dual kinase inhibitor of c-Src and c-Abl kinases." Bioorg Med Chem. 13(15):4704-12.

Chen T, George JA, Taylor CC. (2006) "Src tyrosine kinase as a chemotherapeutic target: is there a clinical case?" Anticancer Drugs;17(2):123-31.

Product Citations:

Yayama K, Sasahara T, Ohba H, Funasaka A, Okamoto H. (2014) "Orthovanadate-induced vasocontraction is mediated by the activation of Rho-kinase through Src-dependent transactivation of epidermal growth factor receptor." Pharmacol Res Perspect. 2014 Apr;2(2):e00039. doi: 10.1002

Neuber S, Jäger S, Meyer M, Wischmann V, Koch PJ, Moll R, Schmidt A. (2015) "c-Src mediated tyrosine phosphorylation of plakophilin 3 as a new mechanism to control desmosome composition in cells exposed to oxidative stress." Cell Tissue Res. 2015 Mar;359(3):799-816.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.