| Identification | Back Directory | [Name]
(5-METHOXY-1H-INDOL-2-YL)PHENYLMETHANONE | [CAS]
74588-78-6 | [Synonyms]
D-6413
CS-888
D-64131
D 64131; D64131
D-64131(sc-203908)
(5-METHOXY-1H-INDOL-2-YL)PHENYLMETHANONE
Methanone,(5-methoxy-1H-indol-2-yl)phenyl- | [Molecular Formula]
C16H13NO2 | [MDL Number]
MFCD04039791 | [MOL File]
74588-78-6.mol | [Molecular Weight]
251.28 |
| Chemical Properties | Back Directory | [Melting point ]
162 °C | [Boiling point ]
455.2±25.0 °C(Predicted) | [density ]
1.231±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
Soluble in DMSO | [form ]
Crystalline solid | [pka]
14.81±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Novel inhibitor of tubulin polymerization | [Definition]
ChEBI: (5-methoxy-1H-indol-2-yl)-phenylmethanone is a N-acylindole. | [Biological Activity]
Novel inhibitor of tubulin polymerization; cytotoxic and inhibits tumor cell proliferation in vitro (IC 50 = 74 nM). Prevents growth of tumor models in mice following oral administration in vivo . | [in vivo]
D-64131 (200-400 mg/kg; p.o.; daily; days 1-5, 8-9, and 15-18) significantly inhibits tumor growth in the human amelanoic melanoma MEXF 989 tumor xenograft mice model[1].
D-64131 has oral bioavailability and is well tolerated at efficacious doses[1].
| Animal Model: | Outbred nude mice (6-8 weeks), human amelanoic melanoma MEXF 989 tumor xenograft model[1] | | Dosage: | 200 mg/kg, 400 mg/kg | | Administration: | Oral administration, daily, on days 1-5, 8-9, and 15-18 after xenograft | | Result: | Resulted in significant tumor growth inhibition during treatment. |
| [References]
1. beckers t, reissmann t, schmidt m et al. 2-aroylindoles, a novel class of potent, orally active small molecule tubulin inhibitors. cancer res. 2002 jun 1;62(11):3113-9. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
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