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SKLB 610

Name: SKLB 610
Brand: Selleck Chemicals
SKU: S6526
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Catalog No.S6526

For research use only.

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.

CAS No. 1125780-41-7

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VEGFR Signaling Pathway Map

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]

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 (from reference)

Animal Research: ^[1]	Animal Models: Female BALB/c nude mice implanted with HCT116 and A549 cells Dosages: 50 mg/kg/day Administration: IP

References

[1] Cao ZX, et al. Cell Physiol Biochem. 2011, 27(5):565-74.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	415.37
Formula	C₂₁H₁₆F₃N₃O₃
CAS No.	1125780-41-7
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F

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