1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. SKLB1002

SKLB1002 

Cat. No.: HY-13944 Purity: 98.04%
Handling Instructions

SKLB1002 is a potent VEGFR2 inhibitor with an IC50 of 32 nM.

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

SKLB1002 Chemical Structure

SKLB1002 Chemical Structure

CAS No. : 1225451-84-2

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Description

SKLB1002 is a potent VEGFR2 inhibitor with an IC50 of 32 nM.

IC50 & Target[1]

VEGFR2

32 nM (IC50)

In Vitro

SKLB1002 inhibits VEGF-induced VEGFR2 phosphorylation and activation of various downstream signaling substrates that are responsible for endothelial cell viability. SKLB1002 inhibits HUVEC proliferation, migration, invasion, and tube formation. SKLB1002 effectively induces cell growth inhibition of L-02 cells at concentrations over 150 μM. SKLB1002 significantly inhibits endothelial cell proliferation with an IC50 value of 11.9 μM. 10 μM SKLB1002 significantly suppresses the phosphorylation of VEGFR2, ERK, FAK, and Src induced by VEGF, which suggests that SKLB1002 exerts its antiangiogenic function by directly targeting VEGFR2 on the surface of endothelial cells and further antagonizing VEGFR2-mediated downstream signaling cascade[1].

In Vivo

SKLB1002 strongly antagonizes the initiation of intersegmental vessels sprouting with no or least impact on normal cell proliferation in the zebrafish embryos. 100 mg/kg SKLB1002 significantly suppresses tumor volume and causes more than 60% inhibition of tumor growth compared with vehicle-treated mice. Tumor angiogenesis is inhibited in mice treated with SKLB1002, which participates in suppression of tumor growth.[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.625 mg/mL (17.56 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1212 mL 15.6060 mL 31.2120 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL
10 mM 0.3121 mL 1.5606 mL 3.1212 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Kinase inhibition is measured by the use of radiometric assays. Briefly, in the presence or absence of SKLB1002, VGFR2 (5-10 mU) is incubated in 25-μL reaction solution containing 8 mM 3-(N-morpholino)propanesulfonic acid (MOPS), pH 7.0, 0.2 mM EDTA, 0.33 mg/mL myelin basic protein, 10 mM Mg acetate, and γ-[33P]ATP. After incubation for 40 minutes at room temperature, the reaction is stopped and 10 μL of the reaction solution is then spotted onto a P30 filtermat and washed 3 times for 5 minutes in 75 mM phosphoric acid and once in methanol prior to scintillation counting[1].

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

Cell Assay
[1]

Cell proliferation is measured using MTT assay. Various cells including HUVECs, L-02, B16-F10, HepG2, and SW620 are treated with indicated concentrations of SKLB1002 (0-10 μM) for 24 hours. Vandetanib and sunitinib served as positive controls. Each assay is replicated 3 times[1].

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

Animal Administration
[1]

Mice: SW620 and HepG2 tumors are established. After 10 days, mice bearing tumors around 100 mm3 are selected and randomized into treatment groups (6 mice per group). The dosing schedules are SKLB1002 100 mg/kg/d, 50 mg/kg/d, or vehicle once a day intraperitoneally. Tumor length and width are determined every 3 days and tumor volume (TV) is calculated. At the end of experiment, mice are sacrificed. Solid tumors are removed and processed for immunohistochemical analysis and terminal deoxynucleotidyl transferase–mediated dUTP nick end labeling (TUNEL) assay[1].

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

References
Molecular Weight

320.39

Formula

C₁₃H₁₂N₄O₂S₂

CAS No.

1225451-84-2

SMILES

CC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SKLB1002
Cat. No.:
HY-13944
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SKLB1002

Cat. No.: HY-13944