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Chemical Structure| 1225451-84-2 Chemical Structure| 1225451-84-2

Structure of SKLB1002
CAS No.: 1225451-84-2

Chemical Structure| 1225451-84-2

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SKLB1002 is a potent inhibitor of VEGF receptor 2 signaling.

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Product Details of SKLB1002

CAS No. :1225451-84-2
Formula : C13H12N4O2S2
M.W : 320.39
SMILES Code : CC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1
MDL No. :MFCD27938707
InChI Key :RQVGFDBMONQTBC-UHFFFAOYSA-N
Pubchem ID :71461003

Safety of SKLB1002

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SKLB1002

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR2

    VEGFR2, IC50:32 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human umbilical vein endothelial cells (HUVECs) 10 or 50 nM 24 hours To assess the effect of SKLB1002 on VEGF-induced proliferation, migration, and tube formation in HUVECs, results showed significant inhibition of these functions PMC7185286
Human umbilical vein endothelial cells (HUVECs) 1 to 100 nM 48 hours To evaluate the cytotoxicity of SKLB1002 on HUVECs, results showed no obvious cytotoxicity at concentrations ranging from 1 to 100 nM PMC7185286
HCT116 cells 10 ng/mL 24 hours SKLB1002 inhibited the ability of HCT116 cells to form tube-like structures and reduced VE-cadherin expression. PMC5577671

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR mice Alkali-burn corneal model Eyedrop 0.05 mg/ml 3 times per day for 7 days To evaluate the inhibitory effect of SKLB1002 on corneal neovascularization, results showed significant reduction in the number and length of new blood vessels PMC7185286
Rats Type 2 diabetic GK rat model Intraperitoneal injection 10 mg/kg body weight Once daily for 2 weeks To inhibit VEGFR-2 activation, increase ROBO4 expression, and reduce cerebral neovascularisation PMC5342922
Nude mice HCT116 xenograft model Intraperitoneal injection 100 mg/kg/d Once daily for 30 days SKLB1002 significantly inhibited tumor growth, reduced necrotic areas, and decreased VE-cadherin expression. PMC5577671

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.21mL

6.24mL

3.12mL

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