Sunitinib MalateAn antineoplastic agent, Flk-1 inhibitor, and ATP-competitve inhibitor of PDGFRβ

Sunitinib Malate (CAS 341031-54-7)

Sunitinib Malate | CAS 341031-54-7 is rated 5.0 out of 5 by 1.
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Synonym: SU-11248
Application: An antineoplastic agent, Flk-1 inhibitor, and ATP-competitve inhibitor of PDGFRβ
CAS Number: 341031-54-7
Purity: ≥97%
Molecular Weight: 532.56
Molecular Formula: C26H33FN4O7
* Refer to Certificate of Analysis for lot specific data (including water content).

Sunitiba Malate is an antineoplastic agent and a potent RTK inhibitor which includes Flk-1 (VEGFR2) as a primary target. It also is a potent, ATP-competitive inhibitor of VEGFR, PDGFR-β and c-Kit (KIT). Sunitiba Malate inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models. Sunitinib Malate is an inhibitor of c-Fms-CSF-1R, Flt-1, Flt-3/Flk-2, Flt-4, PDGFR-α and Ret.


References

Sun, L., et al.: J. Med. Chem., 46, 1116 (2003), Mendel, D.B., et al.: Clin. Cancer Res., 9, 327 (2003), Sistla, A., et al.: Drug Dev. Ind. Pharm., 30, 19 (2004), Sakamoto, K.M., et al.: Curr. Opin. Invest. Drugs, 5. 1329 (2004),

Physical State :
Solid
Solubility :
Soluble in water (>25 mg/ml, pH 1.2-6.8), DMSO (>10 mg/ml), and methanol.
Storage :
Store at 4° C
Melting Point :
185-192° C
Refractive Index :
n20D ~1.61 (Predicted)
IC50 :
VEGFR2: IC50 = 80 nM; PDGFRβ: IC50 = 2 nM; wild-type FLT3: IC50 = 250 nM; FLT3-ITD: IC50 = 50 nM; FLT3-Asp835: IC50 = 30 nM; VEGF-induced proliferation of serum-starved HUVEC50s: IC50 = 40 nM; PDGFRα: IC50 = 69 nM; MV4;11: IC50 = 8 nM; OC1-AML5: IC50 = 14 nM; CSF1R: IC50 = 0.012 µM
Ki Data :
VEGFR -1: Ki= 2 ; VEGFR -2: Ki= 9 ; VEGFR -3: Ki= 17 ; PDGFRβ: Ki= 8 ; KIT: Ki= 4
pK Values :
pKa: 8.95
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
PubChem CID :
6456015
Merck Index :
14: 9000
MDL Number :
MFCD08282795
SMILES :
CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C.C([C@@H](C(=O)O)O)C(=O)O

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Certificate of Analysis

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Sunitinib Malate  Product Citations

See how others have used Sunitinib Malate. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 25002903  Chen, J. et al. 2014. Evidence-based complementary and alternative medicine : eCAM. 2014: 484269.

PMID: # 23781255  Ho, JY. et al. 2013. Evid Based Complement Alternat Med. 2013: 161628.

PMID: # 23047550  2012. Br. J. Cancer. 107: 1702-13.

PMID: # 22791880  2012. Clin. Cancer Res. 18: 4549-59.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Ferguson Ferguson, MJ. et al. (PubMed 26375012) assessed proliferation, -hexosaminidase release (degranulation), and Erk1/2 phosphorylation in Sunitinib Malate, an antineoplastic, multi-kinase inhibitor, treated Nf1+/- mast cells and fibroblasts. Sunitinib Malate suppressed multiple in vitro gain-in-functions of Nf1+/- mast cells and fibroblasts and attenuated Erk1/2 phosphorylation. -SCBT Publication Review
Date published: 2015-03-13
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