Chemodex

Sunitinib malate

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Product Details
Synonyms Sunitinib L-malate; SU112248; N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (2S)-2-hydroxybutanedioic acid (1:1) salt
Product Type Chemical
Properties
Formula C22H27FN4O2 . C4H6O5
MW 532.56
CAS 341031-54-7
RTECS UX9356900
Source/Host Chemicals Synthetic
Purity Chemicals ≥98% (HPLC)
Appearance Yellow, orange to brown powder.
Solubility Soluble in DMSO (10mg/ml).
Identity Determined by 1H-NMR.
Declaration Manufactured by Chemodex.
Other Product Data

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Our product description may differ slightly from the original manufacturers product datasheet.

InChi Key LBWFXVZLPYTWQI-IPOVEDGCSA-N
Smiles CC1=C(/C=C2C(NC3=C\2C=C(F)C=C3)=O)NC(C)=C1C(NCCN(CC)CC)=O.O[C@H](C(O)=O)CC(O)=O
Shipping and Handling
Shipping AMBIENT
Short Term Storage +20°C
Long Term Storage +20°C
Handling Advice Protect from light and moisture.
Use/Stability Stable for at least 2 years after receipt when stored at RT.
Documents
Product Specification Sheet
Datasheet Download PDF
Description
Sunitinib malate is a potent ATP-competitive and cell permeable multi-targeted receptor tyrosine kinase (RTK) inhibitor targeting VEGFR, PDGFR-β and c-Kit (Ki = 2-17nM). It inhibits FLK1 (Ki=9nM), PDGFRβ (Ki=8nM) and FLT3. It is at least 10-fold selective for FLK1 and PDGFRβ over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl and Src. Sunitinib malate inhibits the cellular receptor phosphorylation of FLT3, RET and CSF-1R. Sunitinib malate exhibits potent antiangiogenic and antitumor activity in multiple xenograft models. It decreases VEGF- and FGF-induced proliferation of human umbilical vein endothelial cells (HUVECs) and reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 20 to 80 mg/kg per day.
Product References
(1) L. Sun, et al.; J. Med. Chem. 46, 1116 (2003) | (2) D. B. Mendel, et al.; Clin. Cancer Res. 9, 327 (2003) | (3) A.M. O'Farrell, et al.; Blood 101, 3597 (2003) | (4) J. Guo, et al.; Mol. Cancer. Ther. 5, 1007 (2006) | (5) E.D. Deeks & G.M. Keating; Drugs 66, 2255 (2006) | (6) S. Faivre, et al.; Nat. Rev. Drug Discov. 6, 734 (2007) | (7) R. Roskoski; BBRC 356, 323 (2007)
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