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| | SKLB1002 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;CS-1002;SKLB 1002; SKLB-1002;Quinazoline, 6,7-dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]-;SKLB1002 USP/EP/BP | | CAS: | 1225451-84-2 | | MF: | C13H12N4O2S2 | | MW: | 320.39 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1225451-84-2.mol |  |
| | SKLB1002 Chemical Properties |
| Melting point | 193 °C | | Boiling point | 522.4±60.0 °C(Predicted) | | 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 | | form | powder to crystal | | pka | -0.14±0.30(Predicted) | | color | White to Light yellow |
| | SKLB1002 Usage And Synthesis |
| Uses | SKLB1002 is a potent vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor that inhibits angiogenesis and tumor growth in vivo. | | 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]. | | target | VEGFR2 | | 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. |
| | SKLB1002 Preparation Products And Raw materials |
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