| Identification | Back Directory | [Name]
SKLB1002 | [CAS]
1225451-84-2 | [Synonyms]
CS-1002
SKLB1002
SKLB1002 USP/EP/BP
SKLB 1002; SKLB-1002
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
Quinazoline, 6,7-dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]-
6,7-Dimethoxy-4-[(5-methyl-1,3,4-thiadiazol-2-yl)thio]quinazoline SKLB 1002 | [Molecular Formula]
C13H12N4O2S2 | [MDL Number]
MFCD27938707 | [MOL File]
1225451-84-2.mol | [Molecular Weight]
320.39 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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