| Identification | Back Directory | [Name]
R-1530 | [CAS]
882531-87-5 | [Synonyms]
R1530
R-1530
R 1530
R-1521
CS-1111
R 1530, >=98%
R 1530; R-1530
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine
5-(2-Chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine
Pyrazolo[3,4-b][1,4]benzodiazepine, 5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl- | [Molecular Formula]
C18H14ClFN4O | [MDL Number]
MFCD23704870 | [MOL File]
882531-87-5.mol | [Molecular Weight]
356.78 |
| Chemical Properties | Back Directory | [Boiling point ]
550.9±50.0 °C(Predicted) | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble20mg/mL, clear | [form ]
powder | [pka]
17.23±0.40(Predicted) | [color ]
white to yellow to light brown |
| Hazard Information | Back Directory | [Uses]
R 1530 is a multi-kinase inhibitor. It exhibits inhibitory activity against Chk2, KDR, FGFR, Aurora A kinase and Cdk2. It also binds VEGFR-2, FGFR1 and PDGFRβ. It displays antiproliferative activity in vitro and inhibits mitosis and angiogenesis. | [Biological Activity]
R1530 is a multi-kinase inhibitor with activity against several kinases associated with tumor growth and angiogenesis, including VEGFR, FGFR, PDGFR, Chk2 and Cdk2. In tumor cells, R1530 inhibits tubulin polyerization and mitotic checkpoint function, resulting in polyploidy. The compound R1530 inhibits tumor growth and angiogenesis in animal models. | [in vivo]
R1530 (1.56, 25, and 50 mg/kg; p.o.; daily, for 28 days.) has notable antitumor activity across a broad range of human xenograft models, with minimal toxicity[1]. | Animal Model: | Human tumor xenograft models[1] | | Dosage: | 1.56, 25 and 50 mg/kg | | Administration: | Oral administration; daily, for 28 days. | | Result: | Inhibited tumor growth in all models, with regression observed in all models tested at a 50 mg/kg dose. |
| [IC 50]
KDR: 10 nM (IC50); FGFR1: 28 nM (IC50) |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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