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SKLB 610 VEGFR inhibitor

Cat.No.S6526

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.
SKLB 610 VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 415.37

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Quality Control

Batch: S652601 DMSO]83 mg/mL]false]Ethanol]27 mg/mL]false]Water]Insoluble]false Purity: 99.40%
99.40

Chemical Information, Storage & Stability

Molecular Weight 415.37 Formula

C21H16F3N3O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1125780-41-7 -- Storage of Stock Solutions

Synonyms N/A Smiles CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 83 mg/mL ( (199.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 27 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
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].
References

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