SKLB 610

Catalog No.S6526

SKLB 610 Chemical Structure

Molecular Weight(MW): 415.37

SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.

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Biological Activity

Description SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.
Targets
VEGFR2 [1]
()
FGFR2 [1]
()
PDGFR [1]
()
PDGFR [1]
()
FGFR2 [1]
()
In vitro

In vitro, SKLB610 shows selective inhibition of VEGF-stimulated human umbilical vein endothelial cells (HUVECs) proliferation, and this proliferation inhibitory effect is associated with decreased phosphorylation of VEGFR2 and p42/44 mitogen-activated protein kinase (p42/44 MAPK). SKLB610 inhibits a panel of human cancer cells proliferation in a concentration-dependent manner and human nonsmall cell lung cancer cell line A549 and human colorectal cancer cell line HCT116 are most sensitive to SKLB610 treatment. At concentration of 10μM, SKLB610 inhibits 65% FGFR2 activity and 55% PDGFRE activity, respectively. Relative to PDGFR2 and FGFR2 SKLB610 has more selective inhibition of VEGFR2 which shows 97% inhibition of VEGFR2 activity at 10μM in vitro. No inhibition of enzyme activity is detected when 10μM of SKLB610 is examined against PI3K, EGFR, Aurora-A, CDK2/cyclinE and CDK6/cyclinD3[1].

In vivo

In vivo, chronic intraperitoneally administration of SKLB610 at dose of 50mg/kg/d results in significant inhibition in the growth of established human A549 and HCT116 tumor xenografts in nude mice without exhibit toxicity[1].

Protocol

Animal Research:

[1]

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  • Animal Models: Female BALB/c nude mice implanted with HCT116 and A549 cells
  • Formulation: 25% (v/v) aqueous Cremophor EL/ethanol (50:50)
  • Dosages: 50 mg/kg/day
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (199.82 mM)
Ethanol 27 mg/mL (65.0 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.37
Formula

C21H16F3N3O3

CAS No. 1125780-41-7
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID