1225451-84-2

Basic information

• Product Name: SKLB1002
• Synonyms: SKLB1002;2-((6,7-diMethoxyquinazolin-4-yl)thio)-5-Methyl-1,3,4-thiadiazole;6,7-Dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]quinazoline;6,7-Dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]quinazoline SKLB 1002
• CAS NO: 1225451-84-2
• Molecular Formula: C13H12N4O2S2
• Molecular Weight: 320.38998
• Product Categories: Inhibitors
• Mol File: 1225451-84-2.mol
• Article Data: 0

Chemical Properties

• Melting Point: 193 °C
• Boiling Point: 522.4±60.0 °C(Predicted)
• Appearance: /
• Density: 1.45±0.1 g/cm3(Predicted)
• Storage Temp.: Sealed in dry,Store in freezer, under -20°C
• Solubility: insoluble in H2O; ≥5 mg/mL in EtOH with gentle warming and ultrasonic; ≥8 mg/mL in DMSO
• PKA: -0.14±0.30(Predicted)
• CAS DataBase Reference: SKLB1002(CAS DataBase Reference)
• NIST Chemistry Reference: SKLB1002(1225451-84-2)
• EPA Substance Registry System: SKLB1002(1225451-84-2)

Safety Data

• Hazardous Substances Data: 1225451-84-2(Hazardous Substances Data)

Usage

Description

SKLB1002 is a potent vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor, which plays a crucial role in inhibiting angiogenesis and tumor growth in vivo.

Uses

Used in Pharmaceutical Industry:
SKLB1002 is used as an anticancer agent for its ability to inhibit VEGFR2, thereby suppressing angiogenesis and tumor growth. This makes it a promising candidate for the development of cancer therapies targeting the VEGFR2 pathway.
Used in Drug Development:
SKLB1002 is used as a research tool in drug development for the identification and evaluation of potential VEGFR2 inhibitors. Its potent inhibitory activity against VEGFR2 can help researchers understand the underlying mechanisms of angiogenesis and tumor growth, leading to the discovery of novel therapeutic agents.
Used in Cancer Research:
SKLB1002 is used as a research compound in cancer research to study the role of VEGFR2 in angiogenesis and tumor growth. By investigating the effects of SKLB1002 on various cancer cell lines and animal models, researchers can gain insights into the potential therapeutic benefits of targeting VEGFR2 in cancer treatment.

Biological Activity

sklb1002 is a potent inhibitor of vegf receptor 2 with ic50 value of 32 nm [1].vegf receptor 2 (vegfr2) is a major receptor for vascular endothelial growth factor (vegf) and plays an important role in angiogenesis and vegf-stimulated proliferation, migration, and sprouting of cultured endothelial cells [1].sklb1002 is a potent vegfr2 inhibitor. in human umbilical vein endothelial cells (huvec), sklb1002 significantly inhibited vegf-induced huvec proliferation with ic50 value of 11.9 μm. also, sklb1002 inhibited huvec migration, invasion and tube formation in a dose-dependent way. sklb1002 (10 μm) significantly inhibited vegf-induced phosphorylation of vegfr2, erk, src and fak [1].in zebrafish embryos, sklb1002 (2.5 μm) significantly inhibited the growth of intersegmental vessels. in mice bearing sw620 or hepg2 xenografts, sklb1002 (100 mg/kg) significantly inhibited tumor volume and inhibited tumor growth by 60%. also, sklb1002 reduced the microvessel density [1]. in mice with 4t1 tumor, sklb1002 significantly reduced the tumor vessel density [2].

references

[1]. zhang s, cao z, tian h, et al. sklb1002, a novel potent inhibitor of vegf receptor 2 signaling, inhibits angiogenesis and tumor growth in vivo. clin cancer res, 2011, 17(13): 4439-4450. [2]. shen g, li y, du t, et al. sklb1002, a novel inhibitor of vegf receptor 2 signaling, induces vascular normalization to improve systemically administered chemotherapy efficacy. neoplasma, 2012, 59(5): 486-493.