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Chemodex
Sunitinib malate
As low as
271
CHF
CHF 271.00
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CDX-S0330-G0011 gCHF 271.00
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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 |
Click here for Original Manufacturer 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)