1. Protein Tyrosine Kinase/RTK
  2. FGFR
    PDGFR
    VEGFR
  3. SKLB610

SKLB610 

Cat. No.: HY-18199 Purity: 98.96%
Handling Instructions

SKLB610 is a VEGFR inhibitor with potent anti-tumor activity.

For research use only. We do not sell to patients.

SKLB610 Chemical Structure

SKLB610 Chemical Structure

CAS No. : 1125780-41-7

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Description

SKLB610 is a VEGFR inhibitor with potent anti-tumor activity.

IC50 & Target[1]

VEGFR1

 

PDGFR

 

FGFR1

 

In Vitro

SKLB610 has a selective inhibition of VEGF-induced proliferation with an IC50 value of 2.2μM. In HUVECs, SKLB610 shows selectivity of 2-fold for inhibition of VEGF-induced proliferation versus bFGF-induced proliferation with an IC50 value of 4.7μM. In HUVECs, SKLB610 blocks VEGF stimulated phosphorylation of VEGFR2 in a dose dependent manner after SKLB610 treatment. SKLB610 significant inhibits HUVECs capillary tube formation in a concentration-dependent manner. SKLB610 inhibits the formation of vessel-like structures at 2.5 μM[1].

In Vivo

SKLB-610 inhibits tumor xenograft model growth of human non-smallcell lung cancer model (A549) and human colon cancer model (HCT116) and is well tolerated. After 30 days treatment, SKLB610 exhibited a significantly antitumor activity in inhibiting tumor progress compared with control. The inhibition rate of tumor volume in SKLB610-treated groups is 70.2% (50 mg/kg) for A549 and 77.1% (50 mg/kg) for HCT116 [1]. The retention times of SKLB610 and the internal standard are 5.6 and 8.1 min, respectively. The quantification limit is 67 ng/mL. The calibration curves are linear over a concentration range of 0.1–50 µg/mL[2].

Molecular Weight

415.37

Formula

C₂₁H₁₆F₃N₃O₃

CAS No.

1125780-41-7

SMILES

O=C(C1=NC=CC(OC2=CC=C(NC(C3=CC=CC(C(F)(F)F)=C3)=O)C=C2)=C1)NC

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
Kinase Assay
[1]

The inhibitory ability of SKLB610 on kinase activity is determined using labeled γ-P33ATP. Peptide as kinase substrates are monitored by labeled phosphate. Briefly, 10mU human VEGFR2, FGFR2, PDGFR-E EGFR, PI3K, Aurora-A, CDK2/ cyclinE and CDK6/cyclinD3 are incubated with 25μL solution containing SKLB610 or vehicle (8mM MOPS pH 7.0, 0.2mM EDTA, 10mM Mg Acetate, 10μM [γ-P33ATP] and their own peptide as substrate. The reaction is initiated by the addition of the MgATP mix. After incubation for 40 minutes, the reaction is stopped by the addition of 5μL of a 3% phosphoric acid solution. 10 μL of the reaction is then spotted onto a P30 filtermat and washed three times for 5 minutes in 75mM phosphoric acid and once in methanol prior to drying. Finally, kinase activity is detected using scintillation counting method[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

The effect of SKLB610 on cell viability is evaluated by CCK-8 assay. Briefly, cell are seeded in 96-well plates (2000-4000 cells/well) for 24h, followed by SKLB610 treatment at concentrations of 1.25-40 μM for 48h. After the culture period, the supernatant fluid is removed and medium contains 10% CCK- 8 reagent is added for 2-4 h incubation at 37°C. The light absorptions (OD) are measured at 450 nm with microplate spectrophotometer[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Rats: Rats are fasted for 12 h with free access to water before administration and divided randomly into two groups. SKLB610 suspension and SKLB610 solution at a dose of 50 mg/kg SKLB610 are administered. A 250-μL blood sample is collected into heparinized tubes by retro-orbital puncture at 0.083, 0.25, 0.5, 1, 2, 3, 4, 8, 10, 12 and 24 h after a single dose by administration of 50 mg/kg SKLB610. The blood samples are centrifuged at 7,000 rpm for 10 min to obtain the plasma. The plasma samples are stored at -20°C until analysis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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SKLB610
Cat. No.:
HY-18199
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