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Sunitinib Malate

Sunitinib Malate

Product ID S8253
Cas No. 341031-54-7
Purity ≥98%
Product Unit SizeCostQuantityStock
5 mg $78.10 In stock
25 mg $204.30 In stock
100 mg $638.80 In stock
Bulk Quote

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  • Description
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Description

Sunitinib is an inhibitor of several tyrosine kinases, including PDGFR, VEGFR, KIT, and FLT3. Sunitinib also inhibits mTORC1 signaling. Sunitinib is currently clinically used to treat renal cell carcinoma and gastrointestinal stromal tumors, but is in clinical trials as a potential treatment for a variety of other cancers. Sunitinib exhibits anticancer chemotherapeutic, anti-angiogenic, and anti-fibrotic activities. In anaplastic thyroid cancer cells, sunitinib decreases activity of VEGFR2, prevents phosphorylation of EGFR, ERK1/2, and Akt, and suppresses expression of cyclin D1, inhibiting cell proliferation; in paired animal models, this compound inhibits tumor growth. In acute myelogenous leukemia (AML) cells, sunitinib decreases expression of cyclin D1, cyclin D3, cyclin-dependent kinase 2 (CDK2), Bcl-2, and Mcl-1 and increases expression of p27, pRb1, p130, Bax, Bak, Fas, FasL, DR4, DR5, and activated PKC, resulting in activation of caspases 2, 3, 8, and 9 and apoptosis. In endothelial cells, sunitinib inhibits tube formation and vascular sprouting. In animal models, sunitinib decreases cyst area and increases the number of cyst-free subjects, indicating potential benefit in the treatment of endometriosis. Additionally, this compound inhibits collagen synthesis, cell migration, contraction, and cell differentiation of hepatic stellate cells.

Product Info

Cas No.

341031-54-7

Purity

≥98%

Formula

C26H33FN4O7

Formula Wt.

532.56

IUPAC Name

N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene) methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide;(2S)-2-hydroxybutanedioic acid

Synonym

Sutent

Melting Point

194-200°C

Solubility

Soluble in DMSO at 40 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility

Appearance

Brown to Orange Crystal Powder

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

S8253 MSDS PDF

Info Sheet

S8253 Info Sheet PDF

References

Tran TA, Kinch L, Peña-Llopis S, et al. Platelet-derived growth factor/vascular endothelial growth factor receptor inactivation by sunitinib results in Tsc1/Tsc2-dependent inhibition of TORC1. Mol Cell Biol. 2013 Oct;33(19):3762-79. PMID: 23878397.

Di Desidero T, Fioravanti A, Orlandi P, et al. Antiproliferative and proapoptotic activity of sunitinib on endothelial and anaplastic thyroid cancer cells via inhibition of Akt and ERK1/2 phosphorylation and by down-regulation of cyclin-D1. J Clin Endocrinol Metab. 2013 Sep;98(9):E1465-73. PMID: 23969186.

Abbas MA, Disi AM, Taha MO. Sunitinib as an anti-endometriotic agent. Eur J Pharm Sci. 2013 Jul 16;49(4):732-6. PMID: 23747661.

Majumder S, Piguet AC, Dufour JF, et al. Study of the cellular mechanism of Sunitinib mediated inactivation of activated hepatic stellate cells and its implications in angiogenesis. Eur J Pharmacol. 2013 Apr 5;705(1-3):86-95. PMID: 23454556.

Teng CL, Yu CT, Hwang WL, et al. Effector mechanisms of sunitinib-induced G1 cell cycle arrest, differentiation, and apoptosis in human acute myeloid leukaemia HL60 and KG-1 cells. Ann Hematol. 2013 Mar;92(3):301-13. PMID: 23180436.

George S. Sunitinib, a multitargeted tyrosine kinase inhibitor, in the management of gastrointestinal stromal tumor. Curr Oncol Rep. 2007 Jul;9(4):323-7. PMID: 17588358.

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