[CAS NO. 1225451-84-2] SKLB1002
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PRODUCTS SPECIFICATIONS [1225451-84-2]
Store
Catalog
SLK-S7258
Brand
Selleck
CAS
1225451-84-2
DESCRIPTION [1225451-84-2]
Overview
| MDL | MFCD27938707 |
|---|---|
| Molecular Weight | 320.39 |
| Molecular Formula | C13H12N4O2S2 |
| SMILES | CC1=NN=C(SC2=C3C=C(OC)C(OC)=CC3=NC=N2)S1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 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 |
| 50 mM | - | - | - |
Description
SKLB1002 is a potent and ATP-competitive inhibitor with of 32 nM.
Targets
| VEGFR2 [1] |
| 32 nM |
In vitro
SKLB1002 shows strikingly lower cytotoxicity on normal human cells L-02. SKLB1002 significantly inhibits HUVEC proliferation, migration, invasion, and tube formation, by inhibiting VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including ERK, FAK, and Src.
In vivo
In the zebrafish embryos, SKLB1002 remarkably blocks the formation of embryonic and tumor-induced angiogenesis with no or least impact on normal cell proliferation. In athymic mice bearing SW620 or HepG2 xenografts, SKLB1002 (100 mg/kg daily, i.p.) causes significant inhibition of tumor growth, inhibits tumor angiogenesis and induces tumor apoptosis. In 4T1 and CT26 tumor model, SKLB1002 and local hyperthermia produce a synergistic antiangiogenesis, anticancer and promotion of apoptosis efficacy.
References
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